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The year 2021 is a year of rapid progress in clinical research and clinical practice of China's original third-generation EGFR-TKI (Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor) drugs for the treatment of advanced non-small cell lung cancer (NSCLC)
.
Interpretation of the "Three Kingdoms" to achieve a breakthrough In March 2021, a new national first-class drug, fumetinib mesylate (commonly known as "Fu drug" in China), was approved for the treatment of diseases that occurred during or after previous EGFR-TKI treatment.
Adult patients with locally advanced or metastatic NSCLC who have progressed and have EGFR T790M mutation-positive NSCLC
.
Both fumetinib and another Chinese original third-generation EGFR-TKI (almetinib mesylate) have been recommended by China's authoritative lung cancer diagnosis and treatment guidelines for the treatment of EGFR T790M mutation-positive advanced NSCLC
.
Targeted therapy for advanced lung cancer recommended by the Chinese Medical Association Oncology Society Lung Cancer Clinical Diagnosis and Treatment Guidelines (2021 Edition) In January, the results of a phase III clinical study of almetinib in the first-line treatment of Chinese advanced NSCLC with sensitive EGFR mutations showed that the progression-free survival (PFS) reached 19.
3 months, and the risk of disease progression was reduced by 54% [2]
.
In December 2021, the Phase III clinical study of fumetinib in the first-line treatment of EGFR-sensitive mutated advanced NSCLC successfully obtained positive results.
Group can bring significantly longer PFS benefits, PFS is expected to exceed 20 months, and the reduction in the risk of disease progression is expected to achieve new breakthroughs
.
In December 2021, almetinib was approved in China for the first-line treatment of advanced NSCLC with sensitive EGFR mutations
.
In December 2021, fumetinib was included in the national medical insurance reimbursement catalog as the only third-generation EGFR-TKI.
Before medical insurance reimbursement, the monthly treatment cost of fumetinib has decreased by nearly 80%
.
In 2022, the treatment of EGFR mutation-positive advanced NSCLC will have three third-generation EGFR-TKIs "competing on the same stage", and all three drugs have entered the national medical insurance reimbursement catalog through price negotiation
.
How to choose a drug will be an issue for clinicians in 2022
.
On Thursday (January 13), the Chinese Society of Clinical Oncology (CSCO) Foundation held two lectures on targeted therapy for lung cancer, including Professor Cheng Ying from Jilin Provincial Cancer Hospital and Department of Medical Oncology, Shanghai Pulmonary Hospital affiliated to Tongji Medical University.
Prof.
Zhou Caicun, Prof.
Han Baohui from Department of Respiratory Medicine, Shanghai Chest Hospital Affiliated to Jiaotong University, Prof.
Shi Yuankai from Cancer Hospital of Chinese Academy of Medical Sciences, and many other big names in the field of lung cancer treatment in China will share the clinical research results and clinical practice experience of fumetinib, and discuss Clinical selection of third-generation EGFR-TKI drugs
.
The trend of clinical application of third-generation EGFR-TKIs This platform recently interviewed Professor Zhou Caicun, and talked with Professor Zhou about the treatment needs of EGFR mutation-positive NSCLC (including early and mid-term), as well as the clinical application trend of EGFR-TKI drugs
.
Its content sheds light on how to select third-generation EGFR-TKI drugs
.
An excerpt from that interview is shared here for readers
.
Yi Mai Tong: In the era of EGFR-mutated advanced NSCLC gradually becoming a chronic disease, is the safety of targeted therapy drugs particularly prominent? Professor Zhou Caicun's EGFR-TKI drugs have completely changed the treatment pattern of advanced NSCLC with sensitive EGFR mutations, and the patient's survival has also been significantly prolonged.
The median OS has been extended from about 12 months in the era of chemotherapy to 38.
6 in the era of third-generation EGFR-TKIs Within a few months, this type of lung cancer has gradually become a controllable chronic disease
.
However, this also puts forward higher requirements for the safety and tolerability of third-generation EGFR-TKI drugs
.
Because the patient can tolerate "short pain" such as diarrhea and rash, but if it is "long pain", it will affect the quality of life of the patient, and the patient may not be able to tolerate the treatment for a long time
.
Yimaitong: The central nervous system (CNS) is the most common distant metastatic site of advanced lung cancer
.
Does the treatment of lung cancer CNS metastases often require increased drug doses? Professor Zhou Caicun said that with the prolongation of patient survival, the incidence of brain metastases from lung cancer will also be higher than in the era of chemotherapy
.
About 50% of patients develop CNS metastases within three years
.
Therefore, evaluating the efficacy of a lung cancer-targeted drug and the efficiency of treating brain metastases is a very important dimension, because it means that the patient's survival will also take a step forward
.
Compared with the first-generation EGFR-TKI, the third-generation EGFR-TKI can penetrate the blood-brain barrier and enter the brain better.
However, in clinical practice, the treatment of brain metastases or meningeal metastases is like the treatment of rare or rare mutations in EGFR.
The dose of the drug needs to be increased to ensure adequate drug concentrations in the cerebrospinal fluid and brain
.
However, whether the dose can be increased is closely related to the safety and tolerability of the drug
.
In fact, in clinical practice, we have many examples of need to increase the dose of drugs
.
For example, a patient taking 80 mg of osimertinib developed meningeal metastasis.
After we increased the drug dose to 160 mg, we found that the symptoms of meningeal metastasis were under control, but the patient could not stand it because the toxic and side effects such as rash and diarrhea appeared or aggravated; that is to say Increasing the dose of drugs can effectively control brain metastases or meningeal metastases, but whether the dose can be increased depends on how wide the safety window of the drug dose is
.
Yimaitong: Why is the dose safety window of fumetinib so wide? Professor Zhou Caicun innovatively introduced the trifluoroethoxypyridine structure of vormetinib, so that its prototype drug and its main metabolites have high anti-tumor activity, and both of them have highly selective anti-tumor effects
.
In fact, other three-generation EGFR-TKIs are also highly specific for the selection of EGFR mutation targets, but the metabolites after entering the human body lose high selectivity, and can inhibit both EGFR-sensitive mutations and EGFR wild-type.
lead to more adverse reactions
.
Yimaitong: Currently, EGFR-TKI targeted drugs have been approved in China for postoperative adjuvant treatment of patients with early and mid-stage NSCLC
.
Is the safety of targeted therapy drugs more important for postoperative adjuvant therapy? Professor Zhou Caicun's targeted drugs are used in the adjuvant treatment of patients with early and mid-stage lung cancer.
The safety of the drugs determines the success or failure of the final treatment
.
Why is security important? Mainly because patients receiving postoperative adjuvant therapy need to take the drug for a long time.
If the safety and tolerance are good, the disease-free survival (DFS) will definitely be longer, and if the DFS is longer, the overall survival (OS) will naturally be longer.
On the contrary, if the adverse reactions cannot be tolerated, then the treatment cannot be adhered to, and the DFS will naturally be short
.
So this is worth our attention
.
For the postoperative adjuvant treatment of early lung cancer, in addition to rash and diarrhea, we should also pay attention to other uncommon side effects, such as liver function damage, interstitial pneumonia, and gastrointestinal adverse reactions, such as anorexia, stomatitis etc.
_
If these adverse events accumulate to make patients "left behind", the efficacy will naturally be compromised
.
Compared with osimertinib and almetinib, the third-generation EGFR-TKI of BEST, fumetinib is a latecomer
.
However, fumetinib in the treatment of lung cancer, especially lung cancer brain metastases (Brain), has shown excellent efficacy (Efficacy) in clinical research and clinical practice, and its safety (Safety) clinical research data and clinical practice.
Tolerability is impressive
.
In 2021, in view of the characteristics of "dual activity", "double entry into the brain" and "high selectivity" exhibited by vormetinib and its main metabolites, in clinical practice, vormetinib is often used (sometimes).
, double dose) for the treatment of patients with brain metastases from lung cancer with poor efficacy after multi-line therapy, or patients with poor response to osimertinib, or intolerance
.
In 2022, fumetinib, which has entered the national medical insurance reimbursement catalogue, is bound to gain wider clinical application, and only during this process can doctors spy, discover, and perceive what the young Chinese "forbidden medicine" can show.
Characteristics of BEST's third-generation EGFR-TKI
.
References: [1] Oncologists Branch of Chinese Medical Doctor Association, Medical Oncology Branch of China Association for the Promotion of International Exchange of Health Care.
Chinese Treatment Guidelines for Stage IV Primary Lung Cancer (2021 Edition) [J].
Chinese Journal of Oncology 2021,43(1) :39-59, DOI:10.
3760/cma.
j.
cn112152-20201009-00884.
[2] Lu S, et al.
Randomized phase Ⅲ trial of aumolertinib (HS-10296, Au) versus gefitinib (G) as first-line treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) and EGFR exon 19 del or L858R mutations (EGFRm).
ASCO 2021.
Abstr 9013
.
Interpretation of the "Three Kingdoms" to achieve a breakthrough In March 2021, a new national first-class drug, fumetinib mesylate (commonly known as "Fu drug" in China), was approved for the treatment of diseases that occurred during or after previous EGFR-TKI treatment.
Adult patients with locally advanced or metastatic NSCLC who have progressed and have EGFR T790M mutation-positive NSCLC
.
Both fumetinib and another Chinese original third-generation EGFR-TKI (almetinib mesylate) have been recommended by China's authoritative lung cancer diagnosis and treatment guidelines for the treatment of EGFR T790M mutation-positive advanced NSCLC
.
Targeted therapy for advanced lung cancer recommended by the Chinese Medical Association Oncology Society Lung Cancer Clinical Diagnosis and Treatment Guidelines (2021 Edition) In January, the results of a phase III clinical study of almetinib in the first-line treatment of Chinese advanced NSCLC with sensitive EGFR mutations showed that the progression-free survival (PFS) reached 19.
3 months, and the risk of disease progression was reduced by 54% [2]
.
In December 2021, the Phase III clinical study of fumetinib in the first-line treatment of EGFR-sensitive mutated advanced NSCLC successfully obtained positive results.
Group can bring significantly longer PFS benefits, PFS is expected to exceed 20 months, and the reduction in the risk of disease progression is expected to achieve new breakthroughs
.
In December 2021, almetinib was approved in China for the first-line treatment of advanced NSCLC with sensitive EGFR mutations
.
In December 2021, fumetinib was included in the national medical insurance reimbursement catalog as the only third-generation EGFR-TKI.
Before medical insurance reimbursement, the monthly treatment cost of fumetinib has decreased by nearly 80%
.
In 2022, the treatment of EGFR mutation-positive advanced NSCLC will have three third-generation EGFR-TKIs "competing on the same stage", and all three drugs have entered the national medical insurance reimbursement catalog through price negotiation
.
How to choose a drug will be an issue for clinicians in 2022
.
On Thursday (January 13), the Chinese Society of Clinical Oncology (CSCO) Foundation held two lectures on targeted therapy for lung cancer, including Professor Cheng Ying from Jilin Provincial Cancer Hospital and Department of Medical Oncology, Shanghai Pulmonary Hospital affiliated to Tongji Medical University.
Prof.
Zhou Caicun, Prof.
Han Baohui from Department of Respiratory Medicine, Shanghai Chest Hospital Affiliated to Jiaotong University, Prof.
Shi Yuankai from Cancer Hospital of Chinese Academy of Medical Sciences, and many other big names in the field of lung cancer treatment in China will share the clinical research results and clinical practice experience of fumetinib, and discuss Clinical selection of third-generation EGFR-TKI drugs
.
The trend of clinical application of third-generation EGFR-TKIs This platform recently interviewed Professor Zhou Caicun, and talked with Professor Zhou about the treatment needs of EGFR mutation-positive NSCLC (including early and mid-term), as well as the clinical application trend of EGFR-TKI drugs
.
Its content sheds light on how to select third-generation EGFR-TKI drugs
.
An excerpt from that interview is shared here for readers
.
Yi Mai Tong: In the era of EGFR-mutated advanced NSCLC gradually becoming a chronic disease, is the safety of targeted therapy drugs particularly prominent? Professor Zhou Caicun's EGFR-TKI drugs have completely changed the treatment pattern of advanced NSCLC with sensitive EGFR mutations, and the patient's survival has also been significantly prolonged.
The median OS has been extended from about 12 months in the era of chemotherapy to 38.
6 in the era of third-generation EGFR-TKIs Within a few months, this type of lung cancer has gradually become a controllable chronic disease
.
However, this also puts forward higher requirements for the safety and tolerability of third-generation EGFR-TKI drugs
.
Because the patient can tolerate "short pain" such as diarrhea and rash, but if it is "long pain", it will affect the quality of life of the patient, and the patient may not be able to tolerate the treatment for a long time
.
Yimaitong: The central nervous system (CNS) is the most common distant metastatic site of advanced lung cancer
.
Does the treatment of lung cancer CNS metastases often require increased drug doses? Professor Zhou Caicun said that with the prolongation of patient survival, the incidence of brain metastases from lung cancer will also be higher than in the era of chemotherapy
.
About 50% of patients develop CNS metastases within three years
.
Therefore, evaluating the efficacy of a lung cancer-targeted drug and the efficiency of treating brain metastases is a very important dimension, because it means that the patient's survival will also take a step forward
.
Compared with the first-generation EGFR-TKI, the third-generation EGFR-TKI can penetrate the blood-brain barrier and enter the brain better.
However, in clinical practice, the treatment of brain metastases or meningeal metastases is like the treatment of rare or rare mutations in EGFR.
The dose of the drug needs to be increased to ensure adequate drug concentrations in the cerebrospinal fluid and brain
.
However, whether the dose can be increased is closely related to the safety and tolerability of the drug
.
In fact, in clinical practice, we have many examples of need to increase the dose of drugs
.
For example, a patient taking 80 mg of osimertinib developed meningeal metastasis.
After we increased the drug dose to 160 mg, we found that the symptoms of meningeal metastasis were under control, but the patient could not stand it because the toxic and side effects such as rash and diarrhea appeared or aggravated; that is to say Increasing the dose of drugs can effectively control brain metastases or meningeal metastases, but whether the dose can be increased depends on how wide the safety window of the drug dose is
.
Yimaitong: Why is the dose safety window of fumetinib so wide? Professor Zhou Caicun innovatively introduced the trifluoroethoxypyridine structure of vormetinib, so that its prototype drug and its main metabolites have high anti-tumor activity, and both of them have highly selective anti-tumor effects
.
In fact, other three-generation EGFR-TKIs are also highly specific for the selection of EGFR mutation targets, but the metabolites after entering the human body lose high selectivity, and can inhibit both EGFR-sensitive mutations and EGFR wild-type.
lead to more adverse reactions
.
Yimaitong: Currently, EGFR-TKI targeted drugs have been approved in China for postoperative adjuvant treatment of patients with early and mid-stage NSCLC
.
Is the safety of targeted therapy drugs more important for postoperative adjuvant therapy? Professor Zhou Caicun's targeted drugs are used in the adjuvant treatment of patients with early and mid-stage lung cancer.
The safety of the drugs determines the success or failure of the final treatment
.
Why is security important? Mainly because patients receiving postoperative adjuvant therapy need to take the drug for a long time.
If the safety and tolerance are good, the disease-free survival (DFS) will definitely be longer, and if the DFS is longer, the overall survival (OS) will naturally be longer.
On the contrary, if the adverse reactions cannot be tolerated, then the treatment cannot be adhered to, and the DFS will naturally be short
.
So this is worth our attention
.
For the postoperative adjuvant treatment of early lung cancer, in addition to rash and diarrhea, we should also pay attention to other uncommon side effects, such as liver function damage, interstitial pneumonia, and gastrointestinal adverse reactions, such as anorexia, stomatitis etc.
_
If these adverse events accumulate to make patients "left behind", the efficacy will naturally be compromised
.
Compared with osimertinib and almetinib, the third-generation EGFR-TKI of BEST, fumetinib is a latecomer
.
However, fumetinib in the treatment of lung cancer, especially lung cancer brain metastases (Brain), has shown excellent efficacy (Efficacy) in clinical research and clinical practice, and its safety (Safety) clinical research data and clinical practice.
Tolerability is impressive
.
In 2021, in view of the characteristics of "dual activity", "double entry into the brain" and "high selectivity" exhibited by vormetinib and its main metabolites, in clinical practice, vormetinib is often used (sometimes).
, double dose) for the treatment of patients with brain metastases from lung cancer with poor efficacy after multi-line therapy, or patients with poor response to osimertinib, or intolerance
.
In 2022, fumetinib, which has entered the national medical insurance reimbursement catalogue, is bound to gain wider clinical application, and only during this process can doctors spy, discover, and perceive what the young Chinese "forbidden medicine" can show.
Characteristics of BEST's third-generation EGFR-TKI
.
References: [1] Oncologists Branch of Chinese Medical Doctor Association, Medical Oncology Branch of China Association for the Promotion of International Exchange of Health Care.
Chinese Treatment Guidelines for Stage IV Primary Lung Cancer (2021 Edition) [J].
Chinese Journal of Oncology 2021,43(1) :39-59, DOI:10.
3760/cma.
j.
cn112152-20201009-00884.
[2] Lu S, et al.
Randomized phase Ⅲ trial of aumolertinib (HS-10296, Au) versus gefitinib (G) as first-line treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) and EGFR exon 19 del or L858R mutations (EGFRm).
ASCO 2021.
Abstr 9013
