Drug intelligence / Profile preview

dasatinib + ruxolitinib + trametinib + capivasertib + venetoclax

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This entity represents an investigational multi-agent targeted therapy combination comprising dasatinib (a BCR-ABL/Src family tyrosine kinase inhibitor), ruxolitinib (a Janus kinase 1/2 inhibitor), trametinib (a MEK1/2 inhibitor), capivasertib (an AKT inhibitor), and venetoclax (a BCL-2 inhibitor). Each component is an orally available small-molecule targeted anticancer drug: dasatinib and ruxolitinib have been explored together to co-inhibit BCR-ABL and JAK/STAT signaling in Philadelphia chromosome–positive acute lymphoblastic leukemia, while trametinib targets MAPK pathway signaling at MEK, capivasertib blocks PI3K–AKT pathway signaling, and venetoclax antagonizes the anti-apoptotic protein BCL-2 to promote mitochondrial apoptosis.[4][5][6][8] This five‑drug combination is not an approved, standardized regimen but conceptually represents an aggressive pathway‑centric strategy to simultaneously inhibit BCR-ABL, JAK/STAT, MAPK/ERK, PI3K–AKT, and BCL‑2 survival signaling in hematologic or solid malignancies where these pathways are co‑activated.

02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)BCL-2 (BCL-2 family)JAK2 (Janus kinase 2)SFK (SRC family kinases)AKT2 (Rac-beta serine/threonine-protein kinase)JAK1 (Janus kinase 1)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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