Drug intelligence / Profile preview

avapritinib + vincristine + dactinomycin

Development stage
Unknown
Lead developer
Blueprint Medicines
Modality
Small Molecules
Administration
Oral (avapritinib), Intravenous (vincristine), Intravenous (dactinomycin)
01

Overview

This is a **combination regimen** consisting of **avapritinib**, **vincristine**, and **dactinomycin**. - **Avapritinib** is a potent, selective small molecule inhibitor of oncogenic KIT and PDGFRA kinases, primarily targeting mutations associated with gastrointestinal stromal tumors (GIST) and systemic mastocytosis. Its primary mechanism is the inhibition of the active conformation of KIT and PDGFRA kinases, particularly KIT D816V and PDGFRA D842V mutations, leading to decreased tumor cell proliferation and survival[1][3][4][5][10]. - **Vincristine** is a vinca alkaloid chemotherapy agent that inhibits microtubule formation in mitotic spindles, arresting cell division in metaphase via tubulin binding and disruption[2]. - **Dactinomycin** (actinomycin D) is an antitumor antibiotic that intercalates into DNA and inhibits RNA synthesis, thereby preventing cell proliferation. This specific three-drug combination is not a standard or widely studied regimen, and while all three agents are independently approved and used in various antineoplastic protocols, there are no prominent references to this exact three-drug combination being clinically investigated or approved as a unified regimen. Each drug brings a distinct antitumor mechanism: receptor tyrosine kinase inhibition, mitotic arrest, and transcriptional inhibition.

Other names
avapritinib + vincristine + dactinomycin
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)DNATUBB (Tubulin (alpha and beta subunits))

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