Avapritinib
Vue déterministe de l'entité source de la LJAM. L'autorité clinique demeure avec les ID de la source cités et l'état d'approbation de l ́examinateur.
| ID | DRUG-AVAPRITINIB |
|---|---|
| Type | Médicament |
| Alias | AyvakitAyvakytАваприніб |
| État | reviewed 2026-04-27 | pending_clinical_signoff |
| Maladies | DIS-GIST DIS-MASTOCYTOSIS |
| Sources | SRC-NCCN-GIST-2025 SRC-NCCN-SM-2025 |
Faits sur les drogues
| Catégorie | Type-I selective KIT/PDGFRA inhibitor (D816V- and D842V-active) |
|---|---|
| Mécanisme | Selective KIT and PDGFRA inhibitor designed to bind the active conformation; uniquely active against the imatinib-resistant KIT D816V (advanced systemic mastocytosis) and PDGFRA D842V (GIST) activation-loop mutations. NAVIGATOR (PDGFRA D842V GIST) ORR ~88%; EXPLORER + PATHFINDER (advanced SM) ORR ~75% with deep molecular responses. |
| Dose typique | PDGFRA D842V GIST: 300 mg PO once daily on empty stomach. Advanced systemic mastocytosis: 200 mg PO once daily on empty stomach (lower dose to mitigate cognitive / cerebral microbleed risk seen at 300 mg in EXPLORER). |
| Ukraine enregistrée | Faux |
| NSZU remboursé | Faux |
| Ukraine vérifiée pour la dernière fois | 2026-04-27 |
Avertissements
- Hémorragie intracrânienne / microsanglements cérébraux — dose-dépendante; surveillance de l'IRM initiale + sur le traitement dans le SM avancé
Notes
Two distinct dose levels by indication. NAVIGATOR established 300 mg as PDGFRA D842V GIST dose (transformative ORR ~88% vs <5% historical imatinib in this genotype). EXPLORER showed cognitive AEs and cerebral microbleeds at 300 mg in advanced SM, leading to PATHFINDER's 200 mg dose registration. Baseline + on-treatment brain MRI recommended in advanced SM. Not effective in KIT D816V- negative advanced SM (rare FIP1L1-PDGFRA myeloid neoplasm with eosinophilia is treated with imatinib instead).
Utilisé par
Protocole thérapeutique
REG-AVAPRITINIB-ADVSM-1L- Avapritinib en monothérapie (mastocytose systémique avancée, 1L; KIT D816V+)REG-AVAPRITINIB-GIST-1L- Avapritinib en monothérapie (GIST avancé/métastatique 1L; PDGFRA D842V)