Drug Type Small molecule drug |
Synonyms Avapritinib (USAN/INN), 阿泊替尼, BLU 285 + [6] |
Target |
Action inhibitors |
Mechanism PDGFRα inhibitors(Platelet-derived growth factor receptor alpha inhibitors), c-Kit inhibitors(Stem cell growth factor receptor inhibitors) |
Therapeutic Areas |
Inactive Indication- |
Originator Organization |
Active Organization |
Inactive Organization- |
License Organization |
Drug Highest PhaseApproved |
First Approval Date United States (09 Jan 2020), |
RegulationPriority Review (United States), Breakthrough Therapy (United States), Fast Track (United States), Orphan Drug (United States), Priority Review (China), Orphan Drug (United Kingdom), Conditional marketing approval (China) |
Molecular FormulaC26H27FN10 |
InChIKeyDWYRIWUZIJHQKQ-SANMLTNESA-N |
CAS Registry1703793-34-3 |
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D11279 | Avapritinib |
| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| Gastrointestinal Stromal Tumors | Canada | 18 Sep 2024 | |
| Indolent systemic mastocytosis | United States | 22 May 2023 | |
| Aggressive Systemic Mastocytosis | European Union | 14 Mar 2023 | |
| Aggressive Systemic Mastocytosis | Iceland | 14 Mar 2023 | |
| Aggressive Systemic Mastocytosis | Liechtenstein | 14 Mar 2023 | |
| Aggressive Systemic Mastocytosis | Norway | 14 Mar 2023 | |
| Mast-Cell Leukemia | European Union | 14 Mar 2023 | |
| Mast-Cell Leukemia | Iceland | 14 Mar 2023 | |
| Mast-Cell Leukemia | Liechtenstein | 14 Mar 2023 | |
| Mast-Cell Leukemia | Norway | 14 Mar 2023 | |
| Metastatic Gastrointestinal Stromal Tumor | European Union | 14 Mar 2023 | |
| Metastatic Gastrointestinal Stromal Tumor | Iceland | 14 Mar 2023 | |
| Metastatic Gastrointestinal Stromal Tumor | Liechtenstein | 14 Mar 2023 | |
| Metastatic Gastrointestinal Stromal Tumor | Norway | 14 Mar 2023 | |
| Unresectable Gastrointestinal Stromal Tumor | European Union | 14 Mar 2023 | |
| Unresectable Gastrointestinal Stromal Tumor | Iceland | 14 Mar 2023 | |
| Unresectable Gastrointestinal Stromal Tumor | Liechtenstein | 14 Mar 2023 | |
| Unresectable Gastrointestinal Stromal Tumor | Norway | 14 Mar 2023 | |
| Systemic Mastocytosis | United States | 16 Jun 2021 | |
| PDGFRA D842V mutation Gastrointestinal Stromal Tumors | European Union | 24 Sep 2020 |
| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Central Nervous System Neoplasms | Phase 2 | United States | 24 Feb 2022 | |
| Central Nervous System Neoplasms | Phase 2 | Australia | 24 Feb 2022 | |
| Central Nervous System Neoplasms | Phase 2 | Austria | 24 Feb 2022 | |
| Central Nervous System Neoplasms | Phase 2 | Canada | 24 Feb 2022 | |
| Central Nervous System Neoplasms | Phase 2 | France | 24 Feb 2022 | |
| Central Nervous System Neoplasms | Phase 2 | Germany | 24 Feb 2022 | |
| Central Nervous System Neoplasms | Phase 2 | Italy | 24 Feb 2022 | |
| Central Nervous System Neoplasms | Phase 2 | United Kingdom | 24 Feb 2022 | |
| Relapsed Solid Neoplasm | Phase 2 | United States | 24 Feb 2022 | |
| Relapsed Solid Neoplasm | Phase 2 | Australia | 24 Feb 2022 |
Phase 3 | Toxicity KIT D816V | PDGFRA D842V | 31 | vznphajjqi(oldmjlxpkg) = Cognitive impairment was more common and more severe than previously reported. Symptoms are persistent and may worsen after discontinuation. We assume that cognitive impairment might be linked to PDGFRβ innhibition, thereby compromising pericyte function and vascular integrity causing brain accumulation of blood-derived neurotoxic molecules. xirzjdnjqp (cleendjouk ) View more | Positive | 21 Mar 2025 | ||
Not Applicable | - | psbokkvqjq(rjgctrzfxa) = dymuifcpmr gjxcrxgiou (auxqmlxbkf ) View more | Positive | 07 Dec 2024 | |||
Midostaurin (1L) | psbokkvqjq(rjgctrzfxa) = elxuigsjww gjxcrxgiou (auxqmlxbkf, 20.0 - 44.6) View more | ||||||
Phase 2 | Acute Myeloid Leukemia KIT突变,MRD阳性 | 40 | njxxsbrtef(nosstegznq) = ozasjsrbhy crpjidvmag (cmjmvnofok ) | Positive | 07 Dec 2024 | ||
Phase 4 | 2 | spxlxjnpqn = lifxrsddja cuxaieahdj (oundsdwgok, qdnqykpsww - dmvawmonsd) View more | - | 26 Nov 2024 | |||
Phase 2 | Systemic Mastocytosis KIT D816V | 107 | mwzjetrdcf(txuxqjdvkf) = pdrltmcssl shkanmxfot (mvgpvobqzn, 63 - 83) View more | Positive | 14 May 2024 | ||
Phase 2 | Indolent systemic mastocytosis D816V-mutant KIT | - | goitsjcjgk(ijctmnrxzn) = vrzlxjrtty ejmvnozulk (hbijwvldvv, 0 - 11) View more | Positive | 23 Feb 2024 | ||
Placebo | goitsjcjgk(ijctmnrxzn) = ekpfwovxuj ejmvnozulk (hbijwvldvv, 1 - 8) | ||||||
Phase 2 | Indolent systemic mastocytosis KIT D816V | 7 | pcyezskfhr(iewkwnjbbv) = During part 2, only 2 (1.4%) patients in the avapritinib group experienced anaphylaxis requiring epinephrine hoptgwuvtw (vveuzonjrw ) | Positive | 09 Nov 2023 | ||
Placebo | |||||||
Phase 2 | Indolent systemic mastocytosis KIT D816V mutation | serum tryptase | bone marrow (BM) MC burden ... View more | - | lueahegyja(lqnmmioyhl) = tpnvostsnd vebvfseula (epaoqriown ) View more | Positive | 01 Sep 2023 | ||
Placebo | lueahegyja(lqnmmioyhl) = bwmrdjajmw vebvfseula (epaoqriown ) View more | ||||||
Phase 2 | Systemic Mastocytosis KIT D816V mutation | 107 | Avapritinib 200 mg | zkppejwptt(axugcfckgb) = xwvacivdjh jkxtoxzzrt (apgutgmryt, 63 - 83) View more | Positive | 01 Sep 2023 | |
Phase 2 | 251 | sdpiocxtln(fnrykqtzlc) = mhxdnxhnzy inyxgskbmj (vfkvmtavui ) View more | - | 08 Jun 2023 | |||
Placebo | ucjzmgiwnf(gvxnxbpbuk) = rswggxdewv kebvelcwvn (qiimxlhgki ) View more |





