Gan Lai will report the clinical and pre-clinical data of four non-alcoholic steatohepatitis pipelines in the form of oral reports or posters at the 2021 American Association for the Study of Liver Disease Annual Meeting

Shanghai, October 13, 2021/PRNewswire/ - Kolly Pharmaceutical Co.

Dr.

Dr.

The abstracts that will be presented at the 2021 American Association for the Study of Liver Diseases Annual Meeting are as follows:

NOVEL, FIRST-IN-CLASS, FATTY ACID SYNTHASE (FASN) INHIBITOR TVB-2640 DEMONSTRATES ROBUST CLINICAL EFFICACY AND SAFETY IN A GLOBAL PHASE 2 RANDOMIZED PLACEBO-CONTROLLED NASH TRIAL (FASCINATE-1) CONDUCTED IN THE US AND CHINA

Report format: Parallel session, oral report abstract number: 141 Conference theme: Parallel session 21: NAFLD and NASH: Clinical trials of new therapies Speaker: Dr.

-TVB-2640 is a once-a-day, first-in-class oral small molecule fatty acid synthase (FASN) inhibitor that can reduce liver fat content and inhibit inflammation and fibrosis pathways

-In a 2:1 ratio, subjects with MRI-PDFF (MRI-PDFF) greater than or equal to 8% and fibrosis (MRE greater than or equal to 2.

-TVB-2640 was well tolerated, no adverse events of grade 3 or above occurred, and no serious adverse events occurred during the treatment

-The pharmacokinetic characteristics of the two groups of patients (50mg dose group) in China and the United States are consistent

-TVB-2640 reduced liver fat content and alanine aminotransferase (ALT) in both Chinese and American populations.

A PHASE Ib STUDY TO EVALUATE THE SAFETY, TOLERABILITY, PHARMACOKINETICS AND PHARMACODYNAMICS OF ASC41, A THR-β AGONIST, FOR 28-DAYS IN OVERWEIGHT AND OBESE SUBJECTS WITH ELEVATED LDL-C, A POPULATION CHATERISTIC OF NAFLD

Report format: poster presentation Abstract number: 1851 Conference theme: NAFLD and NASH: Clinical research presentation time: November 12, 2021, Friday, 6:00-11:55 AM EST Key information:

-The liver-targeted prodrug ASC41 is a small molecule, highly effective and selective thyroid hormone Beta receptor (THR-Beta) agonist.

-In this randomized, double-blind, placebo-controlled clinical study, 20 overweight and obese subjects with low-density lipoprotein cholesterol (LDL-C) greater than 110 mg/dL received ASC41 10mg oral tablet or a placebo The ratio is 3:1, once a day, to evaluate the safety, tolerability, pharmacokinetics and lipid-lowering potential of ASC41 oral tablets

-Compared with placebo, the blood lipid parameters (low density lipoprotein cholesterol, triglycerides, total cholesterol, apolipoprotein, lipoprotein (a)) of patients treated with ASC41 showed clinical significance and statistical significance ( P<0.

-ASC41 is safe and well tolerated, with no serious adverse events (SAEs) and adverse reactions of grade 3 or above

ASC42, A NOVEL NON-STEROIDAL FXR AGONIST, DEMONSTRATES A NORMAL CHOLESTEROL PROFILE AND LACK OF PRURITUS AT THERAPEUTIC DOSES IN A 14-DAY PHASE I RANDOMIZED, DOUBLE-BLIND, PLACEBO CONTROLLED STUDY IN HEALTHY VOLUNTEERS

Report Format: Poster Presentation Abstract Number: 1854 Conference Topic: NAFLD and NASH: Clinical Research Presentation Time: November 12, 2021, Friday, 6:00-11:55 AM Eastern Standard Time Abstract Key Information:

-ASC42 is an oral, highly effective and selective non-steroidal farnesoid X receptor (FXR) agonist, and is currently undergoing clinical development for NASH indications

-64 healthy volunteers (8 cohorts, 8 people per cohort (6 ASC42 and 2 placebo)), using 5-200mg ASC42 or placebo (single-dose escalation) and once a day for 14 days 5 -50mg ASC42 or placebo (multi-dose escalation) to evaluate the safety and tolerability of ASC42, and to establish the pharmacokinetic and pharmacodynamic characteristics of ASC42

-During the 14-day treatment, using the human body effective dose of 15 mg, no symptoms of itching were observed

-Within the effective dose range, the 14-day ASC42 treatment showed good safety and tolerability, and there was no increase in alanine aminotransferase (ALT)/aspartate aminotransferase (AST) or blood lipid parameters Abnormal situation
.

-Fibroblast growth factor 19 (FGF19), a biomarker activated by FXR, increased by as much as 1632% on the 14th day of administration (15 mg once a day)
.

-The biomarker 7Alpha-Hydroxy-4-cholesten-3-one (C4), a biomarker activated by FXR, decreased by up to 93% on the 14th day of administration (15mg once a day)
.

-Based on the results of the study, 15 mg once a day has been selected as one of the three doses in the Phase II clinical trial of ASC42 non-alcoholic steatohepatitis
.

ASC43F TABLET AS A ONE-PILL, ONCE-A-DAY FIXED-DOSE COMBINATION (FDC) OF ASC41, A THR-β AGONIST, AND ASC42, AN FXR AGONIST, DEMONSTRATED COMPARABLE DISSOLUTION PROFILES AND IN VIVO PHARMACOKINETICS VS.
ASC41 AND SINGLE ASC41 TABLET

Report format: poster presentation Abstract number: 1762 Conference theme: NAFLD and NASH: Basic research presentation time: November 12, 2021, Friday, 6:00-11:55 AM EST Key information:

-ASC43F is a one-day fixed compound preparation (FDC) composed of ASC41 (an oral liver-targeted THR-Beta agonist prodrug) and ASC42 (a non-steroidal, highly selective, oral FXR agonist) )
.

-In a crossover study design, three male beagle dogs were fed with ASC42 tablets (15mg), ASC41 tablets (5mg) and ASC43F tablets (ASC42/ASC41 15mg/5mg) with a washout period of 5 days.
Assess in vivo pharmacokinetics
.
The test also compared the dissolution curves of ASC43F tablets with the dissolution curves of single ASC41 and ASC42 tablets
.

-In beagle dogs, the pharmacokinetic (PK) parameters of ASC42 and ASC41A derived from ASC43F tablets are consistent with ASC42 and ASC41 monolithic tablets
.

-In 4 different dissolution media with different pH levels, the dissolution profiles of ASC41 and ASC42 in ASC43F tablets are comparable to the dissolution profiles of ASC41 and ASC42 single tablets
.

-Stability research data shows that the ASC43F film remains stable for 4.
5 months under accelerated conditions at a temperature of 40 degrees Celsius and a humidity of 75% (equivalent to 1.
5 years under normal conditions)
.

About songli

Golly is an innovative R&D-driven biotechnology company listed on the Hong Kong Stock Exchange (1672.
HK)
.
Gale is committed to the R&D and commercialization of innovative drugs in the fields of steatohepatitis, tumors (lipid metabolism and oral checkpoint inhibitors), viral diseases, etc.
, to address the clinical needs of patients at home and abroad
.
Under the leadership of a management team with deep professional knowledge and outstanding past achievements, Gerry has developed into an integrated platform company, covering the complete value chain from new drug discovery and development to production and commercialization
.
Gale has three commercialized products and a robust and innovative R&D pipeline:

1.
Non-alcoholic steatohepatitis: Gan Lai Pharmaceutical, a wholly-owned subsidiary of Golly Pharmaceuticals Co.
, Ltd.
, focuses on the development and commercialization of innovative drugs in the field of non-alcoholic steatohepatitis
.
Gan Lai Pharmaceutical has three clinical-stage drug candidates for fatty acid synthase (FASN), thyroid hormone Beta receptor (THR-Beta) and farnesoid X receptor (FXR) and three fixed-dose compound preparations
.
2.
Tumor (lipid metabolism and oral checkpoint inhibitors): focus on the pipeline of oral fatty acid synthase inhibitors that play a key role in tumor lipid metabolism and a new generation of checkpoint inhibitors-oral PD-L1 small molecule inhibitors Pipeline
.
3.
viral diseases: (1) Hepatitis B: Hepatitis B song ceremony focused on the functional development of innovative medicines to cure
.
Explore the subcutaneous injection of PD-L1 antibody ASC22 and Pegasys ® is the cornerstone of the drug, in combination with other targets for drug treatment programs, it is expected to bring a major breakthrough to cure hepatitis B functionality
.
(2) Hepatitis C: Golly successfully developed and marketed two new class 1 drugs, Ganovo® and Xinlilai®, to form a full oral hepatitis C treatment plan
.
(3) AIDS: ASC22 is a kind of immunotherapy, used for AIDS-specific immune reconstruction, and ultimately achieve functional cure of AIDS-infected patients
.

Source: Golly Pharmaceutical Co.
, Ltd.