-
Categories
-
Pharmaceutical Intermediates
-
Active Pharmaceutical Ingredients
-
Food Additives
- Industrial Coatings
- Agrochemicals
- Dyes and Pigments
- Surfactant
- Flavors and Fragrances
- Chemical Reagents
- Catalyst and Auxiliary
- Natural Products
- Inorganic Chemistry
-
Organic Chemistry
-
Biochemical Engineering
- Analytical Chemistry
- Cosmetic Ingredient
-
Pharmaceutical Intermediates
Promotion
ECHEMI Mall
Wholesale
Weekly Price
Exhibition
News
-
Trade Service
Gastrointestinal mesothelioma (GIST) is a common interleuage-based tumor in the gastrointestinal tract, imatinib, schonithinib and rigoffinib are GIST's first, second and third-line therapeutic drugs, respectively, but PDGFRA exon 18 mutations, especially D842V mutation patients are insensitive to existing targeted drugs, the group of patients treatment drugs are scarce.
Based on the analysis of these mutant kinase configurations, the researchers developed the powerful, highly selective I. type KIT and PDGFRA mutation inhibitor Apotheni, which, unlike previous TKI drugs, has strong inhibitory effects on KIT D816V and PDGFRA D842V mutation kinases, adding new options for GIST treatment.
I. Phase NAVIGATOR results confirmed its excellent efficacy, and its high objective remission rate (ORR) was encouraging in patients with D842V mutations.
in the NAVIGATOR study, Apotheni demonstrated good efficacy and safety in the treatment of patients with PDGFRA exon 18 mutations.
reported at the 2019 annual meeting of the American Society of Clinical Oncology (ASCO), the ORR in patients with 18 mutations in PDGFRA exons reached 86% and the ORR in first-line treatment reached 100%.
July 2020, the NAVIGATOR study was published in the international academic journal Lancet Oncology, and Apotony was used for PDGFRA D842V mutant advanced GIST patients with ORR of 88%, of which 9% reached full remission (CR).
in addition, patients with D842V mutations who received Apothesis treatment showed lasting clinical benefits: 12-month continuous remission rate was 70%, 12-month progression-free survival (PFS) was 81%, 24-month total survival (OS) rate was 81%, and Apothetony was generally well-to-do.
2020 ESMO updated the therapeutic effect of D842V mutation GIST, and the data bright eye in the dose climbing and dose expansion queue of the NAVIGATOR I. phase study, a total of 56 patients with PDGFRA D842V mutation were treated with Apotheni <300mg, 300mg, 400 mg, respectively.
analysis of patients in all dosage groups showed that the ORR of Apotony reached 91%, that orR was similar in different dose groups, and that orR reached 96% in patients who received a starting dose of 300 mg.
separately analyzed 5 patients who had not previously been treated with tyrosine kinase inhibitors (TKI), received 300/400 mg of apothetic, 2 obtained CR, and 3 obtained partial remission (PR).
At the same time, patients with effective treatment were able to obtain long-term disease control, patients treated with 300/400 mg, with a medium duration of remission (DOR) of 22 months, a medium PFS of 24 months, and a medium OS of 36 months, 34% and 71%, respectively.
safety analysis showed that the safety of Apotoni 300mg/400mg for patients with D842V mutation was similar to that of the overall population in the NAVIGATOR study.
early 2020, based on NEVIGATOR research data, Apotheteri was approved by the FDA for the treatment of adult patients with PDGFRA exon 18 mutations that cannot be removed or metastasis GIST, bringing life to this group of patients.
, two applications for adaptation certificates for Apotony for advanced adult patients with GIST have also been accepted by the NMPA.
, Apotony filled in the problem of PDGFRA 18 exon mutations, especially in patients with D842V mutations that were not available.
for patients with this type of mutation, Apotheni can be used for full-line treatment.
same time, Apotheni offers new hope for backline therapy in advanced GIST patients, and high remission rates offer the opportunity for re-surgery in advanced patients.
look forward to the future Apoatini continues to be a thorn in the side, in the fight against GIST to make more progress.
source: 1. Heinrich M, Jones R L, von Mehren M, et al. Clinical activity of Avapritinib in ≥ fourth-line (4L+) and PDGFRA Exon 18 gastrointestinal stromal tumors (GIST). 2019 ASCO, abstract 11022.2.Heinrich MC, Jones RL, von Mehren M, et al. Avapritinib in advanced PDGFRA D842V-mutant gastrointestinal stromal tumour (NAVIGATOR): a multicentre, open-label, phase 1 trial[J]. Lancet Oncol, 2020,21(7):935-946.3.Http://clinicalTrials.gov. Accessed August 27, 2018.4.Robin LJ,Cesar S,Margaret VM,et al. Long-term efficacy, tolerability and overall survival in patients with unresectable or metastatic PDGFRA D842V-mutant gastrointestinal stromal tumor treated with avapritinib: NAVIGATOR phase 1 trial update. 2020 ESMO, presentation ID 1621MO.