dasatinib

Overview

Dasatinib is a second-generation BCR-ABL1/Src-family tyrosine kinase inhibitor that also inhibits KIT and PDGFR. It is FDA-approved for chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia. In the UCLA sarcoma PDTO screen it was included in the >400-compound panel and showed sensitivity association with disease trajectory.

Evidence in the corpus

  • In the UCLA sarcoma PDTO biobank (sarcoma_ucla_2024, n=194 specimens), PDTOs from patients with progressive disease at follow-up were more resistant to dasatinib (p=0.039) than those from patients without disease progression — linking dasatinib ex vivo resistance to an aggressive clinical trajectory in sarcoma. PMID:39305899
  • Nominated for KIT-mutated/amplified Triple-WT melanoma subtype (14% of TCGA cases; no hot-spot BRAF/RAS/NF1) alongside imatinib; KIT and co-amplified PDGFRA/KDR at 4q12 provide rationale for KIT inhibitor strategies in this subgroup PMID:26091043
  • In 101 pediatric high-risk oncology patients (PIPseq), dasatinib added to third-line induction for a NUP214-ABL1 BCR-ABL1-like B-cell ALL patient produced deep remission enabling curative bone-marrow transplant PMID:28007021
  • Proposed as a therapeutic for DDR2-overexpressed tumors harboring TRABD–DDR2 promoter-swap fusions, identified in one HNSC sample in the TCGA pan-cancer fusion atlas (n=9,624); DDR2 fusions were detected in nine additional samples across five cancer types PMID:29617662

Resistance mechanisms

  • Progressive clinical disease trajectory is associated with ex vivo PDTO resistance to dasatinib (p=0.039) in sarcoma, alongside sirolimus/rapamycin (p=0.014) and gefitinib (p=0.048). PMID:39305899

Cancer types (linked)

  • OS, LMS, RMS, CHDM — sarcoma subtypes in the pan-sarcoma PDTO screen.

Sources

  • PMID:39305899 — Al Shihabi et al. (Cell Stem Cell 2024). UCLA sarcoma PDTO biobank; dasatinib ex vivo resistance associated with progressive disease at clinical follow-up.

This page was processed by crosslinker on 2026-05-14. - PMID:26091043

This page was processed by crosslinker on 2026-05-14. - PMID:28007021 — Oberg et al. 2017, PIPseq; dasatinib added to third-line induction in NUP214-ABL1 BCR-ABL1-like B-cell ALL, producing deep remission enabling curative BMT. - PMID:29617662 — Gao et al. 2018, Cell Reports. TCGA pan-cancer fusion atlas (n=9,624); dasatinib proposed for DDR2-overexpressed tumors with TRABD–DDR2 promoter-swap fusion in HNSC.

This page was processed by entity-page-writer on 2026-05-15.