Directly hit the drug resistance, China's first third-generation BCR-ABL inhibitor Orebatib was approved!

Directly hit the drug resistance, China's first third-generation BCR-ABL inhibitor Orebatib was approved!

On November 25, 2021, China's National Drug Administration (NMPA) announced the approval of the third-generation BCR-ABL inhibitor Aoarebati, developed by Guangzhou Shunjian Biomedical Technology Co., Ltd. Guangzhou Shunjian Biomedical Technology Co., Ltd. Product Name: Tolera®), used to treat any tyrosine kinase inhibitor (TKI) resistance, and use a fully verified detection method to diagnose chronic myeloid leukemia (CML) with T315i mutation or Adult patients accelerated.

Orebatini is an innovative medicine in which my country has developed and has independent intellectual property rights, and has obtained special support for national "major new drug creation". This means that Orebatib has become the first in China, and the only third-generation BCR-ABL inhibitor solves the major problems of drug-resistant medical treatment in patients with drug-resistant chrometric patients.

As the main researchers of Orebatini China Clinical Trial, the director of the School of Hematology, Peking University, Professor Huang Xiaojun, director of the Blood Department of Peking University People's Hospital, hosted by the China Medical Innovation Promotion Association, the "major new drug creation" "Special Achievements Released and Oarebatini's global starting listing," The effectiveness and safety data of past clinical studies continue to show us that Orebatini is not yet satisfied in drug-resistant chronic myeloid leukemia. The potential of demand is huge, and it is very hoped to become the 'Best-in-class' drug treated in this field. I am very happy to witness the successful list of Orebatib, because this means that China CML treatment is broken. It has ushered in a new milestone drug, which is huge for clinicians and patients. "

CML is a malignant tumor formed by clonality of bone marrow hematopoietic stem cells. According to data, the global incidence is 1.6 / 100,000 ~ 2 / 100,000, and my country's incidence is not optimistic about 0.39 / 100,000 ~ 0.55 / 100,000, China CML patients are more young than Western patients, the median age is 45-50 years old, and the West is 67 years old. A generation of TKI as a first-line treatment of drugs for the 10-year survival rate of CML to 85% ~ 90%, and second-generation TKI first-line treatment allows CML patients to get faster and deeper molecularcal reactions. Despite this, the acquisition resistance has always been CML treatment. The main challenge, there are still some patients who lead to disease progression or even death.

BCR-ABL kinase district mutation is one of the important mechanisms of acquiring resistance, wherein T315i mutation is one of the common drug-resistant mutation types, with about 25% in the drug resistance CML. Patients with T315i mutations were resistant to all generations and second-generation BCR-ABL inhibitors. The third-generation BCR-ABL inhibitor Orebatini is a small molecular protein tyrosine kinase inhibitor, which can effectively inhibit Bcr-ABL tyrosine activation and a variety of mutant activity, which can inhibit BCR-ABL. The phosphorylation of tyrosine kinase and the lower protein STAT5 and CRKL, block downstream pathway activation, induces BCR-ABL positive, BCR-ABLT315i mutant cell line cell cycle blocking and flipping.

According to data released earlier, China's first-phase clinical study, 100 patients with CML, including 86 patients with chronic (CML-CP), and patients with 86 cases (CML-AP). The use of Orebatib is oral, daily administration, 28 days into one cycle, total exploration of a total of 11 dose groups from 1 mg to 60 mg.

The results show that in the CML-CP subject, the baseline does not achieve alleviated can be evaluated, complete hematological relief rate (CHr) is 100%, and the complete cell genetic relief rate (CCYR) is 70%, mainly Molecular Learning Rate (MMR) is 55%. A CHR rate in the CP subject carrying only T315i mutations was 100%, the MCyR rate was 90%, the CCyR rate was 84%, the MMR rate was 78%, the MMR4.0 rate was 68%, and the MR4.5 rate was 58%;

Among the CML-AP subjects, the baseline did not achieve alleviated, CHR was 92%, CCYR was 43%, and the main molecular macrification rate (MMR) was 43%. The CHR ratio in an AP subject carrying only T315i mutations was 67%, the MCyR rate was 60%, and the CCyR rate was 60%, the MMR rate was 60%, and the MMR4.0 rate was 60%, MR4.5 rate. 40%.

In terms of security, most of the adverse events associated with treatment are 1 or 2, and the adverse events can be resumed by suspending administration, reducing the treatment dose or gives support for treatment. As a result, Orebati's CML-CP or CML-AP subjects in TKi-resistant CML-CP or CML-AP have a good tolerance and strong, more sustained antitumor effect. It is worth mentioning that as the fastest heavy product of Ausheng Medicine Listing, Orebati's clinical progress has been selected in the fourth consecutive year, fully showing the efficacy and safety of international hematics. Sex recognition.

Dr. Ceo Yang Dajun, Dr. CEO, said that "Yasheng first approved core product Orebatini is filling domestic gap, clinically indispensable products, effectively solved China's T315i mutation This major social demand problem with drug-resistant patients with drug-resistant patients, let the movie "I am not a medicine god", the society is no longer happening. In the future, we will continue to adhere to "solving China and global patients have not yet met. The mission of clinical demand, bringing more original new drugs that meet clinical needs. I hope that in the near future, Orebati is originally created, the world's leading innovative drug can benefit more patients. "In order to enhance the availability and affordability of Orebatib, it is understood that Ausheng Medicine has reached a strategic cooperation with Cinda's organism in July this year, one of the cooperation contents is that both parties will in China. Joint development and commercialization of Orebatib. In addition, ASIS Pharmaceuticals and Genetic Testing companies, Internet medical enterprises, etc.

With the listing of the third generation BCR-ABL inhibitor, it is expected that China's local innovation forces achieve corner overtaking, let the world know that China has not lagging behind. In any case, CML treatment is about to usher in a new change, Orebati's listing will benefit global patients. It is reported that Orebatib will further globalize. Currently, an open bridge test is being carried out in the United States, which is designed to assess the pharmacokinetics of adult subjects of CML and PH + ALL, an adult subject with T315i mutations. Learning, security and effectiveness. The use of Orebatib is oral, given the next day.


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3. Chinese diagnosis and treatment guidelines for chronic myeloid leukemia (2020 edition). Chinese Journal of Hematology. 2020, 41 (5): 353-364.

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