2022 inventory of 227 IND varieties declared for the first time for domestic Class 1 new drugs, Hengrui leading, Qilu, East Sunshine...

In the past three years, the development of innovative drugs in China has ushered in a phased climax
.
After the first annual IND added more than 100 varieties, it quickly exceeded 200 in just 2 years, and the domestic innovative drug market soon appeared a "volume" phenomenon
.

With the changes in the environment caused by the epidemic in recent years, although the number of new IND varieties of Class 1 new drugs in 2022 is still large, the trend has stabilized, and the development of new drugs and the capital market are gradually calming down, while also better reflecting the current situation
of domestic new drug development at this stage.

01 In 2022, 227 new IND varieties will be added to the first class of domestic chemical drugs

The number of new varieties of Class 1 new drugs in China is one of the important data to measure the
progress of China's innovative drug research and development in 2022.

After the number of new varieties of chemical drugs Class 1 new drugs registered exceeded 100 for the first time in 2019, the rapid growth rate in 2020 and 2021 was almost 50%, and the number of new varieties of chemical drugs Class 1 INDs in 2021 was 243
.

After the explosive momentum of new drug development, the pace of development is gradually slowing down and leveling off
.
As of December 26, 2022 (the full text is counted at this time), through the statistics of Class 1 varieties (chemical drugs) declared for domestic new drug registration and determined one by one, the number of new domestic chemical drug Class 1 varieties in 2022 should be 227.

Figure 1 Statistics of the first declaration of Class 1 IND of Chinese chemical drugs - accepted varieties from 2019 to 2022

Data source: PharmaSmart Data

02 In 2022, Hengrui will lead the way

In the dimension of sponsors, only from the perspective of registered reporting enterprises (not associated with sub-parent companies), the enterprise with the largest number of new IND varieties registered and declared in China in 2022 is Shandong Shengdi, with a total of 7 varieties
.

The following reporting companies are Qilu Pharmaceutical, Jiangsu Hengrui, Dongguang Pharmaceutical, Sino-US Huashitong Biotechnology, Shengshi Techtech Biotechnology, Guangzhou Bibet Pharmaceutical, Jiangsu Enhua and so on
.

In addition, Hengrui Pharmaceutical has outstanding achievements, and this year Hengrui (including Guangdong Hengrui, Jiangsu Hengrui, Shandong Shengdi, Chengdu Shengdi) has about 14 varieties declared IND for the first time, which should be the enterprise
with the largest number of new varieties of chemical drug IND this year.

Figure 2 Enterprises with a large number of IND applications for domestic Class 1 chemical drugs in 2022

Data source: PharmaSmart Data

03 First declaration for the whole year of 2022 - IND varieties accepted

The IND stage varieties of new drugs are based on the different development strategies of the sponsors, and the degree of external disclosure is also different
.
Through the query, the key information of some newly added varieties is further extracted below (in chronological order).

       ● NO.
1：GNP

The development company is Guangzhou Renn Kangya Biomedical Technology Co.
, Ltd.
, and the clinical indications should be pulmonary hypertension and heart failure combined with pulmonary hypertension
.
GNP is a cyclic structure composed of 17 amino acids connected by cysteine disulfide bonds from the venom glandular tissue
of the East African green mamba.

       ● NO.
2：HSK36273

The development company is Haisco Pharmaceutical Group Co.
, Ltd.
, intravenous administration, clinically intended for hemodialysis and intraoperative systemic anticoagulation
.
As a small molecule highly selective factor XIa inhibitor, HSK36273 has the characteristics of
high efficiency, fast onset and fast dissociation.
Studies have shown that it is as effective as heparin and has a better
safety profile.

       ● NO.
3：SCR-6920

The development company is Jiangsu Simcere Pharmaceutical Co.
, Ltd.
, which is an oral protein arginine methyltransferase 5 (PRMT5) inhibitor, which is an antitumor drug in the field of synthetic lethality, and the clinical indication is advanced malignant tumor
.
This variety has high inhibitory activity and high selectivity of PRMT5, and the pharmacokinetic has confirmed that it is easy to distribute in tumors, and the ratio of intratumor drug concentration to plasma drug concentration is about 10 times that of other PRMT5 inhibitors under investigation, which is expected to reduce target-related blood toxicity
.

       ● NO.
4：AC682

The development company is Bingzhoushi Biotechnology (Shanghai) Co.
, Ltd.
, and the target is ER, which is a PROTAC product
.
This variety has received clinical approval from the US FDA for ER+/HER2-locally advanced/metastatic breast cancer
.

       ● NO.
5：FHND5071

The development company is Jiangsu Chia Tai Fenghai Pharmaceutical Co.
, Ltd.
, a RET selective inhibitor with better in vivo efficacy characteristics, higher tumor tissue distribution and lower effective dose, and can also penetrate the blood-brain barrier, which has potential efficacy
for tumors that are primary or metastasized to the central nervous system.

       ● NO.
6：DAJH-1050766

The development company is Chengdu Diao Jiuhong Pharmaceutical Factory, which is a fourth-generation EGFR inhibitor
.
The structure is similar to that of the second-generation ALK inhibitor bucatinib and the fourth-generation EGFR inhibitor BPI-361175
.

       ● NO.
7：SMP-100

The development company is Kelingyuan Biotechnology (Shenzhen) Co.
, Ltd.
, which is a selective serotonin 3 (5-HT3) receptor partial agonist.

This variety can have high affinity and high selectivity with 5-HT3 receptor, good oral pharmacokinetic properties, and low
interaction with other drugs.

       ● NO.
8：QR056251

The development company is Wuhan Langlai Science and Technology Development Co.
, Ltd.
, which is a ROCK inhibitor and is clinically intended for the treatment
of idiopathic pulmonary fibrosis (IPF).

       ● NO.
9：ABSK043

The development company is Shanghai Abbisko Biomedical Technology Co.
, Ltd.
, a PD-L1 inhibitor with high selectivity and good bioavailability, and preclinical data confirm the potent inhibitory effect of this variety and the anti-tumor effect
in multiple preclinical models.

       ● NO.
10：DC05F01

The development company is Beijing Shuanghe Runchuang Technology Co.
, Ltd.
, which is a Fascin protein inhibitor and an anti-tumor oral variety
.
At the same time, this variety is a cross-border innovative drug cooperation project
introduced by CR Shuanghe from NOVITA in the United States through the Innovation Business Department.
It is reported that the relevant R&D projects of this variety have invested at least 149 million yuan
in R&D expenses.

       ● NO.
11：ASC60

The development company is Ascletis Biotechnology (Hangzhou) Co.
, Ltd.
, which is a potent, highly selective and safe oral small molecule fatty acid synthase inhibitor intended for the treatment of advanced solid tumors
.

       ● NO.
12：HHT120

The development company is Shanghai Huahuituo Pharmaceutical Technology Co.
, Ltd.
, which is a targeted thrombin inhibitor intended to be used orally for the prevention of venous thromboembolism
after orthopedic surgery.
At present, the company has invested a total of at least RMB 28.
98 million in R&D expenses in this project
.

       ● NO.
13：QY101

The development company is Qiyuan Biotechnology (Hangzhou) Co.
, Ltd.
, which is a phosphodiesterase 4 (PDE4) inhibitor, which is clinically intended for the treatment
of atopic dermatitis with ointment.
Preclinical trials have preliminarily shown good PK characteristics, good efficacy and safety
.

       ● NO.
14：H002

The development company is Nanjing Hongyun Biotechnology Co.
, Ltd.
, a fourth-generation EGRF inhibitor with broad spectrum and high selectivity against a variety of EGFR mutations, showing extensive and long-lasting antitumor activity in preclinical studies with good
safety profile.

       ● NO.
15：Y-3

The development company is Nanjing Ningdan New Drug Technology Co.
, Ltd.
, which is a new drug
against ischemic stroke.
Y-3 is the only novel structural small molecule PSD-95/nNOS uncoupling agent currently under research in the world, with clear efficacy, good safety, stable pharmacokinetic properties, can penetrate the blood-brain barrier, and has no risk
of degradation by plasmin.

       ● NO.
16：LNK01004

The development company is Linke Pharmaceutical (Hangzhou) Co.
, Ltd.
, which is clinically intended for the treatment
of psoriasis.
It is reported that this variety can simultaneously inhibit multiple inflammatory cytokines and disease-inducing signaling channels associated with psoriasis, and has good efficacy potential
.

       ● NO.
17：HSK36212

The development company is Haisco Pharmaceutical Group Co.
, Ltd.
, which is a small molecule agonist of nuclear factor-related factor pathway independently developed, which is clinically intended to be used for the treatment of chronic renal diseases and kidney diseases
caused by acute kidney injury.

       ● NO.
18：RGT-419B

The development company is Shanghai Qilu Ruige Pharmaceutical R&D Co.
, Ltd
.
, which is clinically expected to improve the safety of currently marketed CDK4/6 inhibitors and overcome drug resistance.
The monodrug activity of this variety, compared with abemaciclib and palbociclib, has a greater
inhibitory effect on ER+ tumor cell growth.

       ● NO.
19：QHL-236

The development company is Shanghai Affinity Biomedical Technology Co.
, Ltd.
, which is a new yew drug with novel structure, which can accumulate and release the efficacy at the tumor site, thereby significantly reducing the toxic side effects of chemotherapy and improving the efficacy
.
It is clinically intended for the treatment
of solid tumors.

       ● NO.
20：BEBT-305

The development company is Guangzhou Bibet Pharmaceutical Co.
, Ltd.
, which is the world's first second-generation HSP90 inhibitor for the oral treatment of psoriasis and other autoimmune diseases, which inhibits autoimmune and inflammatory responses
involved in T cells by downregulating or degrading a variety of cytokines involved in autoimmunity and inflammation.

       ● NO.
21：SYHX2005

The development company is Petrochemical Group Ouyi Pharmaceutical Co.
, Ltd.
, which is a highly selective FGFR4 inhibitor with excellent in vitro and in vivo activity and good safety, and is clinically intended for the treatment
of advanced solid tumors.

       ● NO.
22：XTR006

The development company is Beijing Xiantong International Pharmaceutical Technology Co.
, Ltd.
, which is a radiodiagnostic imaging agent
for positron emission tomography imaging of the brain of Tau protein nerve fiber tangle (NFT).

       ● NO.
23：EVER001

The development company is Genting Xinyao Pharmaceutical Technology Co.
, Ltd.
, which is a new generation of covalent reversible Bruton tyrosine kinase (BTK) inhibitor, which is clinically intended for the treatment of glomerular diseases
.

       ● NO.
24：QR060127

The development company is Wuhan Langlai Science and Technology Development Co.
, Ltd.
, which is a TRPC5 inhibitor, which hinders the detachment of podocytes from the basement membrane by blocking actin remodeling caused by excessive activation of podocytes RAC1 in renal diseases such as FSGS, and maintains the integrity of the glomerular barrier system, and is clinically intended for the treatment
of inflammatory pain and focal stage glomerulosclerosis and other diseases.

       ● NO.
25：XZB-0004

The development company is Xuanzhu Biotechnology Co.
, Ltd.
, which is a highly active and selective AXL-targeted inhibitor, which is clinically intended for the treatment
of advanced solid tumors and hematologic malignancies.

       ● NO.
26：ASK0912

The development company is Jiangsu Aosaikang Pharmaceutical Co.
, Ltd.
, which is an antibacterial drug with broad-spectrum activity against clinically severely resistant gram-negative bacteria (G-), and a number of in vitro and in vitro efficacy studies have shown that the antibacterial activity is stronger than polymyxin B and E, and the toxicity is reduced
.

       ● NO.
27：TRN-157

The development company is Shandong Lukang Pharmaceutical Co.
, Ltd.
, which is a nebulized inhaler clinically intended for the treatment of chronic obstructive pulmonary disease, including chronic bronchitis and emphysema, maintenance treatment of concomitant dyspnea and prevention
of acute attacks.
The project has invested at least 14.
9145 million yuan
.

       ● NO.
28：INS018_055

The development company is Insilico Intelligent Technology (Shanghai) Co.
, Ltd.
, which is the first anti-fibrotic small molecule inhibitor generated by the company based on the AI drug discovery platform for the treatment of idiopathic pulmonary fibrosis
.
Separately, Insilico announced that it has completed the dosing
of multiple subjects INS018_055 phase I clinical trials in Australia.

       ● NO.
29：RP903

The development company is Junshi Runjia (Shanghai) Pharmaceutical Technology Co.
, Ltd.
, which is a PI3K-α inhibitor, which has the potential to inhibit the PI3K pathway and has the effect
of inhibiting cell proliferation.

       ● NO.
30：JDB383

The development company is Shanghai Jiabao Yaoyin Pharmaceutical Technology Co.
, Ltd.
, which is a colony-stimulating factor (CSF1R) inhibitor verified by the first humanized PDX model, which can effectively regulate the survival, proliferation and differentiation
of macrophages.
Preclinical pharmacokinetics showed faster absorption of JDB383 and better bioavailability
.

       ● NO.
31：JS116

The development company is Shanghai Junshi Biomedical Technology Co.
, Ltd.
, which is a small molecule irreversible covalent inhibitor of KRASG12C with a novel structure for the treatment of patients with KRASG12C mutation in non-small cell lung cancer
.
Preclinical studies have shown that JS116 has a wide safety window, good efficacy and safety
.

       ● NO.
30：ceralasertib

The development company is AstraZeneca Global R&D (China) Co.
, Ltd.
, an ATR inhibitor, which has entered clinical phase II~III in the world's highest stage, and the clinical trial
of the drug single agent or combination therapy for a variety of tumors.

       ● NO.
33：WJ13404

The development company is Suzhou Junjing Biomedical Technology Co.
, Ltd.
, a fourth-generation EGFR inhibitor intended for the treatment
of EGFR-mutated non-small cell lung cancer and other solid tumors.

       ● NO.
34：ZKLJ02

The development company is Yunnan Zhongke Longjin Biotechnology Co.
, Ltd.
, which is an anticoagulant whose mechanism of action is to inhibit exposure to key targets FXII and KLK of the kinin system, block coagulation waterfall reaction and inflammatory cascade signaling pathway, and is clinically intended for acute ischemic stroke to improve neurological deficits
.
This variety is derived from forest leeches and synthesized artificially as a peptide candidate
.

       ● NO.
35：CGT-1881

The development company is Shengshi Techtech Biomedical Technology (Suzhou) Co.
, Ltd.
, oral administration, clinically suitable for the treatment
of non-Hodgkin lymphoma or multiple myeloma.

       ● NO.
36：CGT-9475

The development company is Shengshi Techtech Biomedical Technology (Suzhou) Co.
, Ltd.
, which is an anaplastic lymphoma kinase inhibitor, clinically designed to solve drug resistance and central nervous system metastasis, and the cancer still points to non-small cell lung cancer and its brain metastasis
.

       ● NO.
37：HH3806

The development company, Shanghai Haihe Drug Research and Development Co.
, Ltd.
, is a BD2-selective BET inhibitor with inhibitory activity on the BD2 domain more than 200 times
that of BD1.
In animal experiments in preclinical studies, compared with non-selective BET inhibitors, HH3806 retains good efficacy against some solid tumors and hematological tumors, but the killing of normal cells is greatly reduced, and the toxicity of the digestive tract and hematology is significantly reduced
.

       ● NO.
38：NRT6003

The development company is Chengdu Nurett Medical Technology Co.
, Ltd.
, which is a radioactive microsphere for selective internal beam therapy (SIRT), that is, it is obtained by loading high-activity radioactive yttrium [90Y] with carbon microspheres as a carrier, and it is clinically planned to develop the treatment of metastatic liver cancer
.

       ● NO.
39：RFUS-144

The development company is Yichang Renfu Pharmaceutical Co.
, Ltd.
, which is a selective opioid receptor agonist used clinically for the treatment of pruritus
.
Non-clinical research data confirm that it has high affinity and high selectivity, precise analgesic effect, good safety and tolerability, and no adverse reactions
such as addiction, heart, and respiratory depression.

       ● NO.
40：CIGB-814

The development company is Shandong Lukang Pharmaceutical Co.
, Ltd.
, which is a modified peptide ligand of CD4+ T cell epitope of HSP60, which is clinically used for the treatment of rheumatoid arthritis
.

       ● NO.
41：BGM0504

The development company is Borui Biopharmaceutical (Suzhou) Co.
, Ltd.
, which is a dual agonist of GLP-1 and GIP receptor to produce biological effects such as blood sugar control, weight loss and NASH treatment, demonstrating the therapeutic potential
of a variety of metabolic diseases.

       ● NO.
42：RJ4287

Developed by Nanjing Olimes Pharmaceutical Technology Co.
, Ltd.
, it is a novel THRβ selective agonist to improve NASH
by promoting liver lipid metabolism and reducing lipotoxicity.
PS: This breed synchronizes the registration application
of the US FDA.

       ● NO.
43：ICP-490

The development company is Beijing InnoCare Jianhua Pharmaceutical Technology Co.
, Ltd.
, which is a new targeted protein degrader developed through the company's molecular gel platform, that is, by specifically binding to the substrate receptor CRBN of the CRL4 CRBN-E3 ubiquitin ligase complex, it can induce the ubiquitination and degradation of the lymphatic transcription factors Ikaros and Aiolos, thereby inducing apoptosis, and is clinically intended for the treatment of hematological tumors
such as multiple myeloma and non-Hodgkin lymphoma.

       ● NO.
44：WS015

The development company is Sino-US Huashitong Biomedical Technology (Wuhan) Co.
, Ltd.
, which is an innovative polymer drug
that does not absorb orally and does not absorb.
PS: The approval of this variety further proves the innovative research and development capabilities
of Sino-American Huashi Stone in the field of polymer drugs.

       ● NO.
45：HS248

The development company is Hanhui Pharmaceutical Co.
, Ltd.
, which is a highly selective PI3Kγ inhibitor, which can inhibit tumor growth and metastasis by promoting the phenotypic polarization of macrophages to anti-tumor, enhancing the activation of CD8+ T cells in the tumor microenvironment, and is clinically intended to be used in combination with immune checkpoint inhibitors such as PD-1, which is expected to bring more benefits
to patients with PD-1 inhibitor resistance.

       ● NO.
46：HRS-8427

The development company is Jiangsu Hengrui Pharmaceutical Co.
, Ltd.
, which is an antibacterial drug that exerts bacteriostatic and bactericidal effects by inhibiting cell wall biosynthesis, and has been shown to have antibacterial efficacy in mouse infection models constructed from multiple standard strains and clinically isolated strains with good safety in preclinical performance
.
PS: This variety has invested at least about 33.
07 million
yuan in research and development.

       ● NO.
47：HRS-1167

The development company is Jiangsu Hengrui Pharmaceutical Co.
, Ltd.
, which is designed to treat advanced solid tumors by inhibiting the proliferation of tumor cells and exerting anti-tumor effects
.
PS: This variety has invested at least about 18.
79 million
yuan in research and development.

       ● NO.
48：SPN0103-009

The development company, Hangzhou Ausinuo Biotechnology Co.
, Ltd.
, is a novel, long-acting GLP-1 peptide analogue that is clinically intended for the treatment of type 2 diabetes and obesity, and is expected to eventually expand to non-alcoholic fatty liver disease and Alzheimer's disease
.

       ● NO.
49：APS03118

The development company is Beijing Zhijian Jinrui Biomedical Technology Co.
, Ltd.
, which is a highly selective second-generation RET inhibitor, which is clinically intended for the treatment of non-small cell lung cancer, thyroid cancer, pancreatic cancer, breast cancer, ovarian cancer, colorectal cancer and other advanced solid tumors caused by RET gene changes, as well as patients
with drug resistance to first-generation selective RET inhibitors.

       ● NO.
50：WJ-39

The development company is Ningxia Kangya Pharmaceutical Co.
, Ltd.
, which is a quinolinone acetic acid compound designed based on the structure of aldose reductase, a key target of diabetic complications, which is clinically intended for the treatment of diabetic nephropathy and the improvement
of renal function.

       ● NO.
51：HRS-4642

The development company is Jiangsu Hengrui Pharmaceutical Co.
, Ltd.
, which is a KRAS G12D inhibitor that can target KRAS G12D mutations and inhibit tumor cell proliferation, and is the first approved KRAS G12D inhibitor
in China.

       ● NO.
52：HRS-5965

The development company is Chengdu Shengdi Pharmaceutical Co.
, Ltd.
, which can improve glomerular inflammation caused by immune complex deposition, and it has been shown to play a significant therapeutic role in rat nephritis models with good safety in preclinical conditions
.
PS: This variety has invested at least about 27.
2 million yuan in research and development.

● NO.
53: Fluoro[18F] sruin injection

The development company is Shanghai Lannacheng Biotechnology Co.
, Ltd.
, which is a radiological in vivo diagnostic drug targeting PSMA, which has high specificity and affinity with PSMA protein, and is clinically intended for positron emission tomography
imaging of prostate-specific membrane antigen-positive lesions in prostate cancer patients.

       ● NO.
54：BB102

The development company is Beijing Bohui Biotechnology Co.
, Ltd.
, which is a new small molecule kinase inhibitor with high selectivity, novel mechanism of action, effective and safe for gene-mutant tumors, and is clinically intended for the treatment of abnormal gene-driven advanced solid tumors
.

       ● NO.
55：MT1011

The development company, Shaanxi Mekeott Technology Co.
, Ltd.
, is a small molecule broad-spectrum anticoagulant antagonist that is intended to be developed for use in patients receiving anticoagulant therapy (such as factor Xa inhibitors) who need to reverse anticoagulation therapy due to life-threatening or uncontrollable bleeding
.

       ● NO.
56：CG001419

The development company is Shanghai Ruiyue Biotechnology Co.
, Ltd.
, which is a highly selective and potent oral TRK protein degrader, which is clinically intended for NTRK gene fusion, NTRK gene point mutation and NTRK gene amplification or overexpression in advanced or metastatic adult solid tumors
.

       ● NO.
57：Exd391209

The development company is Chengdu Aoda Biotechnology Co.
, Ltd.
, which is a long-acting new hypoglycemic drug intended for the treatment
of type 2 diabetes.
This variety is "upgraded" to the original peptide drug GLP-1 receptor agonist through amino acid long-acting modification technology, and reduces the rate of polypeptide digestion and prolongs the plasma half-life of the drug through the key site of the mutant peptide chain, so as to meet the weekly administration or even biweekly administration
.

       ● NO.
58：SAL0112

The development company is Shenzhen Salubris Pharmaceutical Co.
, Ltd.
, which is an oral small molecule agonist of glucagon-like peptide-1 receptor (GLP-1R), which is clinically intended for the treatment of type 2 diabetes and weight management
in obese or overweight patients.

       ● NO.
59：AC-003

The development company is Econo Biomedical (Suzhou) Co.
, Ltd.
, which is a novel oral small molecule inhibitor targeting receptor interaction protein kinase 1 (RIPK1), which can regulate inflammation and cell death in systemic tissues, and is clinically intended for the treatment
of idiopathic pulmonary fibrosis.

       ● NO.
60：SR750

The development company is Shanghai Thermorod Biotechnology Co.
, Ltd.
, which is an independently developed drug candidate for the treatment of peripheral neuropathic pain, and preclinical studies have shown that SR750 has good safety and pharmacokinetic properties
.

       ● NO.
61：VCT220

The development company is Suzhou Wingtech Pharmaceutical Technology Co.
, Ltd.
, which is a new non-peptide oral small GLP-1 agonist, which can partially restore the function of pancreatic islet β cells, reduce body weight, improve blood lipid profile and lower blood pressure, and the risk of hypoglycemia is small
.
It is clinically intended for the treatment
of type 2 diabetes.

       ● NO.
62：HRS-9821

The development company is Guangdong Hengrui Pharmaceutical Co.
, Ltd.
, which is a bronchial drug that inhibits respiratory tract inflammation and dilates the bronchi, and is clinically intended for the maintenance treatment
of chronic obstructive pulmonary disease.
PS: This variety has invested at least about 23.
25 million
yuan in research and development expenses.

       ● NO.
63：SYHX2009

The development company is Sino-Qi Pharmaceutical Technology (Shijiazhuang) Co.
, Ltd.
, a selective NTRK and ROS1 dual-target inhibitor, which is clinically intended for NTRK or ROS1 gene rearrangement/fusion and its drug-resistant mutation-positive solid tumors
.

       ● NO.
64：HRS-6209

The development company is Jiangsu Hengrui Pharmaceutical Co.
, Ltd.
, which is a selective cell cycle blocker, which can induce G0/G1 phase blockade of tumor cells, and then exert anti-tumor effects, and is clinically intended for the treatment
of advanced malignant tumors.
PS: This variety has invested at least about 30.
14 million
yuan in research and development.

       ● NO.
65：D3S-001

The development company is Desun Ji Pharmaceutical (Wuxi) Co.
, Ltd.
, which is a highly active, highly selective and differentiated KRAS G12C inhibitor with high druggability, strong inhibitory properties, fast inhibition speed, complete invalidation, and good safety and other potential advantages, and is clinically planned to be developed for the treatment of advanced solid tumors
carrying KRAS G12C mutations.

       ● NO.
66：QLH11811

Developed by Qilu Pharmaceutical Co.
, Ltd.
, it is a fourth-generation EGFR inhibitor that reverses C797S mutations and inhibits common ex19del, L858R and T790M
.
In addition, the drug also showed excellent inhibitory activity
against multiple tumor xenognomic models.

       ● NO.
67：EVT-401

The development company is Zhejiang Jinhua Kangbei Biopharmaceutical Co.
, Ltd.
, which is a non-selective cation channel P2X7 inhibitor, which is clinically intended for the treatment
of rheumatoid arthritis.
PS: This variety has invested at least about 22.
8 million
yuan in research and development.

       ● NO.
68：WXSH0208

The development company is Chenxin Pharmaceutical Co.
, Ltd.
, which is an influenza virus RNA polymerase inhibitor, which can block the transcription and replication of viral RNA, inhibit the proliferation of influenza virus, and is clinically intended for the treatment
of influenza A and B.
PS: This variety has invested at least about 49.
4452 million
yuan in research and development expenses.

       ● NO.
69：RBD7022

The development company is Suzhou Ribo Biotechnology Co.
, Ltd.
, which is a self-developed siRNA therapy for ASGPR and PCSK9, which is clinically intended to be used to treat primary (familial and non-familial) hypercholesterolemia or mixed hyperlipidemia
characterized by elevated LDL cholesterol.

       ● NO.
70：Tinlarebant

The development company is Beiliang Biotechnology Pharmaceutical (Shanghai) Co.
, Ltd.
, which is an oral non-tretinoin RBP4 small molecule antagonist, which can reduce and maintain the delivery of vitamin A to the eye to reduce the accumulation of toxic vitamin A byproducts in eye tissue, and is clinically used for the treatment of adolescent hereditary macular degeneration
.

       ● NO.
71：GW201

The development company is Beijing Guangwei Pharmaceutical Technology Co.
, Ltd.
, which is a highly selective and high-affinity NMDA receptor partial agonist, which is clinically planned to be developed for the treatment of depression
.

       ● NO.
72：BGB-15025

BeiGene (Suzhou) Biotechnology Co.
, Ltd.
, developed by BeiGene, is a hematopoietic stem cell kinase 1 (HPK1) inhibitor that inhibits HPK1 effectively promotes T cell activation in preclinical studies, thereby enhancing the antitumor activity
of some clinical PD-1 inhibitors.

       ● NO.
73：HE009

The development company, Nanchang Hongyi Pharmaceutical Co.
, Ltd.
, is an S1P1 small molecule inhibitor intended for the treatment
of systemic lupus erythematosus (SLE).

       ● NO.
74：YZJ-4729

The development company is Shanghai Haiyan Pharmaceutical Technology Co.
, Ltd.
, which is a small molecule drug targeting μ-opioid receptor (MOR), which can activate the MOR receptor
.
In vitro tests have shown that YZJ-4729 has higher selectivity
than TRV130.
In vivo different animal pain models showed dose-dependent potent analgesia, and key respiratory depression and constipation side effects were much weaker than morphine, and significantly better than TRV130
.

       ● NO.
75：ICP-248

The development company is Beijing InnoCare Pharmaceutical Technology Co.
, Ltd.
, which is a new type of highly selective BCL2 inhibitor, which is intended to be used alone or in combination with other drugs such as BTK inhibitors for the treatment of malignant hematological tumors
such as non-Hodgkin lymphoma and acute lymphoblastic leukemia.

       ● NO.
76：BGC1201

The development company is Ganjiang New Area Borui Innovation Pharmaceutical Co.
, Ltd.
, which is an RTK-RAS-MAPK signaling pathway targeted drug intended for the treatment
of advanced solid tumors.

       ● NO.
77：BT-114143

The development company, Sino Hubble Pharmaceutical (Chengdu) Co.
, Ltd.
, is a new small molecule fibrinolytic enzyme/proenzyme inhibitor intended to be used to treat and prevent various bleeding and diseases
caused by hyperfibrinolysis.

       ● NO.
78：RG002

The development company is Shanghai Lingji Biotechnology Co.
, Ltd.
, which is an irreversible pan-FGFR inhibitor with an indication for advanced malignant tumors
.

       ● NO.
79：GH55

The development company is Qinhao Pharmaceutical (Suzhou) Co.
, Ltd.
, which is a dual-mechanism ERK1/2 inhibitor, which inhibits the activation of ERK1/2 by MEK while inhibiting ERK1/2 kinase activity, and is clinically planned to be developed for advanced solid tumors
with mutations in the MAPK signaling pathway.

       ● NO.
80：HT-101

The development company is Suzhou Xingyao Kunze Biopharmaceutical Co.
, Ltd.
, which is a GalNAc-conjugated siRNA innovative drug for clinical use in hepatitis B-related treatment
.

       ● NO.
81：LF0001

The development company is Hangzhou Lingfang Biomedical Technology Co.
, Ltd.
, which is a KRAS G12C inhibitor that is clinically planned for the treatment
of lung cancer, colorectal cancer, pancreatic cancer and other solid tumors with KRAS G12C mutation.

       ● NO.
82：XH-5102

The development company is Shanghai Xunhe Pharmaceutical Technology Co.
, Ltd.
, which is a highly selective JAK2 inhibitor that can be used as a therapeutic drug for autoimmune diseases, and this approval is to develop the treatment of myeloproliferative tumors
.

       ● NO.
83：GFH312

The development company is Zhejiang Jinfang Pharmaceutical Co.
, Ltd.
, which is a RIPK1 inhibitor clinically used in peripheral arterial disease with intermittent claudication
.
This variety has been approved by the US FDA for clinical trials and has completed a Phase I clinical trial
in Australia.

       ● NO.
84：TUL01101

The development company is Zhuhai Federal Pharmaceutical Co.
, Ltd.
, which is a JAK inhibitor topical preparation, which is clinically used for the treatment
of mild to moderate atopic dermatitis.

       ● NO.
85：RAB001

The development company is Zhongshan Laibo Ruichen Biopharmaceutical Co.
, Ltd.
, which is a small molecule polypeptide coupling dual-targeted innovative drug for non-traumatic osteonecrosis, which improves blood circulation, repairs osteonecrosis, and stimulates the formation of
new bone by enhancing endogenous stem cells to target bones.

       ● NO.
86：HBW-3210

The development company is Chengdu Haibowei Pharmaceutical Co.
, Ltd.
, a third-generation BTK inhibitor from the company's brain-penetrating innovative drug development platform, clinically intended for B-cell non-Hodgkin lymphoma, mainly for the development of primary/secondary central nervous system lymphoma or diffuse large B-cell lymphoma
that may involve the central nervous system.

       ● NO.
87：BEBT-503

The development company is Guangzhou Bibet Pharmaceutical Co.
, Ltd.
, which is a highly active pan-PPAR agonist intended for the treatment of diabetes mellitus complicated with nonalcoholic steatohepatitis
.

       ● NO.
88：HRS-1780

The development company is Shandong Shengdi Pharmaceutical Co.
, Ltd.
, which is an oral small molecule drug
clinically intended for the treatment of chronic kidney diseases.
PS: This variety has invested at least about 14.
17 million
yuan in research and development expenses.

       ● NO.
89：TB-D004C

The development company is Shenzhen Tuwei Anchuang Technology Development Co.
, Ltd.
, which is an ultra-long-acting endogenous gastrin regulator analogue, which can act on the dual agonist of human glucagon-like peptide-1 receptor and glucagon receptor at the same time, and is clinically intended for the treatment
of type 2 diabetes.

       ● NO.
90：ATG-037

The development company is Deli (Zhejiang) Pharmaceutical Co.
, Ltd.
, which is an oral CD73 small molecule inhibitor clinically used for the treatment
of locally advanced and metastatic solid tumors.

       ● NO.
91：HRS-1358

The development company is Shandong Shengdi Pharmaceutical Co.
, Ltd.
, which can inhibit the proliferation of tumor cells, overcome target protein mutation resistance and have higher selectivity
for target proteins than traditional small molecule drugs.
PS: This variety has invested at least about 29.
73 million
yuan in research and development expenses.

       ● NO.
92：RGT-264

The development company is Shanghai Qilu Ruige Pharmaceutical R&D Co.
, Ltd.
, which is a highly selective HPK1 (also known as MAP4K1) inhibitor, which is intended for the treatment
of advanced solid tumors.

       ● NO.
93：KMHH-03

The development company is Beijing Kangming Haihui Biotechnology Co.
, Ltd.
, which is a peptide drug, which inhibits the dimerization of protein HER2 receptor by binding to gp96 on the surface of tumor cell membrane, and down-regulates the level of ER-α36 receptor, thereby inhibiting the proliferation of tumor cells, while reducing the stability of uPAR, inhibiting the invasion and metastasis of tumor cells, and is clinically intended for the treatment
of breast cancer.

       ● NO.
94：TR128

The development company is Anhui Zhongke Tuora Pharmaceutical Science Research Co.
, Ltd.
, which is a new generation of pan-RAF kinase inhibitor, in vitro and in vitro experiments have shown that TR128 shows strong inhibition of cell proliferation, induction of apoptosis and other activities of colorectal cancer, pancreatic cancer, non-small cell lung cancer and melanoma with RAS and RAF mutations
.

       ● NO.
95：ASC61

The development company, Ascletis Biotechnology (Hangzhou) Co.
, Ltd.
, is an oral PD-L1 inhibitor whose active metabolite is a potent and highly selective inhibitor that blocks PD-1/PD-L1 interactions
by inducing PD-L1 dimer formation and endocytosis.

       ● NO.
96：IMG-004

The development company is Yingmai Biomedicine (Hangzhou) Co.
, Ltd.
, which is a non-covalent and reversible third-generation BTK inhibitor with potency, high selectivity and brain permeability, and is clinically intended for the treatment
of immune diseases.

       ● NO.
97：AB-218

The development company is Baoyuan Biomedical Technology (Hangzhou) Co.
, Ltd.
, which is an oral selective inhibitor of brain osmotic mutation IDH1, which is well tolerated and well distributed in the brain, and is clinically intended to be used to treat a variety of solid tumors
with IDH1 mutations.

       ● NO.
98：BEBT-607

The development company is Guangzhou Bibet Pharmaceutical Co.
, Ltd.
, which is a highly active KRAS G12C inhibitor, and it is planned to develop single agents and combination drugs for the treatment of KRAS G12C mutated non-small cell lung cancer, colorectal cancer, pancreatic cancer and other solid tumors
.

       ● NO.
99：GMDTC

The development company is Jianersheng (Zhuhai) Pharmaceutical Technology Co.
, Ltd.
, which is a heavy metal poisoning antidote, clinically used to drive away cadmium, lead, platinum and other harmful heavy metals in the human body, can be used for the treatment of cadmium poisoning, can also be used for the treatment of lead poisoning
.

       ● NO.
100：CGT-1967

The development company is Shengshi Techtech Biomedical Technology (Suzhou) Co.
, Ltd.
, which is a CDK4/6 inhibitor intended for the treatment of hematological tumors
.

       ● NO.
101：HJM-353

The development company is Hejing Pharmaceutical Technology (Shanghai) Co.
, Ltd.
, a potent, selective and orally bioavailable EED inhibitor to be developed for the treatment of hematologic malignancies and solid tumors
.

       ● NO.
102：THDBH151

The development company is Dongbao Zixing (Hangzhou) Biopharmaceutical Co.
, Ltd.
, which is a gout dual-target inhibitor, which can not only inhibit xanthine oxidase, but also inhibit the reabsorption of uric acid by the tubular URAT1 transporter, and is clinically intended for the treatment
of gout.

       ● NO.
103：ZX-4081

The development company is Nanjing Zhengxiang Pharmaceutical Co.
, Ltd.
, which is a highly selective PI3Kγ inhibitor, which can be used in combination with immune checkpoint inhibitors such as PD-1/L1 and CTLA4 in clinical combination, and can be used for the resistance of PD1 and CTLA4 inhibitors
.

       ● NO.
104：NH130

The development company, Jiangsu Enhua Pharmaceutical Co.
, Ltd.
, is a potent 5-HT2A receptor reverse agonist, and preclinical test results show that NH130 citrate is effective in animal models of Parkinson's psychiatric disease without affecting motor function
.
PS: The project has invested at least 13 million yuan
in research and development expenses.

       ● NO.
105：TL118

The development company is Suzhou Taoluo Biotechnology Co.
, Ltd.
, which is an anti-tumor new drug for NTRK gene fusion mutations, which is clinically intended for the treatment
of advanced NTRK fusion solid tumors.
This variety has advantages over larotinib and emtricitinib structures and is able to act on the
brain.

       ● NO.
106：NHL35700

The development company is Jiangsu Enhua Pharmaceutical Co.
, Ltd.
, a small molecule phosphodiesterase 10A enzyme inhibitor that can target dopamine receptors, serotonin receptors and adrenergic receptors
.
This variety has a higher affinity for dopamine D1 receptors than D2 receptors, and is expected to reduce the incidence
of side effects such as extrapyramidal reactions and hyperprolactinemia.

       ● NO.
107：[177Lu]Lu-XT033

The development company is Beijing Xiantong International Pharmaceutical Technology Co.
, Ltd.
, which is a radioligand therapy drug
intended for the treatment of adult patients with metastatic prostate cancer positive for prostate-specific membrane antigen.

       ● NO.
108：OAB-14

The development company, Shandong Xinhua Pharmaceutical Co.
, Ltd.
, is a bexarotene derivative that improves Alzheimer's disease-related pathology and cognitive impairment
by increasing the clearance of β-amyloid in APP/PS1 mice.

       ● NO.
109：BPI-460372

The development company, Betta Pharmaceuticals Co.
, Ltd.
, is a new molecular solid compound targeting Hippo signaling pathway 1, which is a novel powerful transcription-enhancing factor TEAD small molecule inhibitor intended for the treatment
of patients with advanced solid tumors.

       ● NO.
110：UA021

The development company is Yusen Jianheng Biopharmaceutical (Shanghai) Co.
, Ltd.
, which is a high-efficiency, highly selective and highly oral bioavailable TYK2 allosteric inhibitor, which is intended to be developed for the treatment of inflammatory bowel disease, psoriasis and other autoimmune diseases
.

       ● NO.
111：AK0706

The development company is Xiamen Tebao Bioengineering Co.
, Ltd.
, which is a new structure of PAPD5/7 small molecule inhibitor, which can inhibit the activity of hepatitis B HBeAg and reduce the expression level of hepatitis B surface antigen, and is clinically intended for the treatment of chronic hepatitis
B.

       ● NO.
112：ECC4703

The development company is Shanghai Chengyi Biotechnology Co.
, Ltd.
, which is a β-selective, liver-targeted THR complete agonist; Preclinical studies have demonstrated efficacy compared to some agonists MGL-3196 and have shown excellent efficacy
in animal models of NASH and dyslipidemia.

       ● NO.
113：BPI-452080

The development company, Betta Pharmaceuticals Co.
, Ltd.
, is an innovative, oral small molecule HIF-2α inhibitor clinically intended for the treatment
of patients with advanced solid tumors.

       ● NO.
114：APG-5918

The development company is Suzhou Ascentage Pharmaceutical Co.
, Ltd.
, which is an oral, new powerful and selective small molecule EED inhibitor; As an allosteric inhibitor, APG-5918 selectively binds to EED proteins, and by modulating tumor epigenetics and tumor microenvironment, it is expected to overcome tumor resistance and achieve complete and durable tumor regression
.

       ● NO.
115：SAL0119

The development company is Shenzhen Salubris Pharmaceutical Co.
, Ltd.
, which is an oral small molecule immunosuppressant with a unique mechanism of action different from JAK class and broad-spectrum cytokine inhibition, and it is planned to develop clinical indications including active ankylosing spondylitis and moderate to severe active rheumatoid arthritis
.

       ● NO.
116：ABSK121-NX

The development company is Wuxi Abbisko Biomedical Technology Co.
, Ltd.
, which is a new generation of oral anti-FGFR resistant mutant inhibitor, which is clinically intended for the treatment of advanced solid tumors
.

Data source: PharmaSmart Data