Drug intelligence / Profile preview

imatinib + cytarabine

Development stage
Phase 3
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous, Intrathecal
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Overview

Imatinib + cytarabine is a combination therapy used primarily in the treatment of chronic myeloid leukemia (CML). Imatinib is a small molecule tyrosine kinase inhibitor that specifically targets the BCR-ABL fusion protein, c-Kit, and platelet-derived growth factor receptor (PDGF-R), thereby inhibiting cancer cell proliferation and survival. Cytarabine is an antimetabolite chemotherapeutic agent that interferes with DNA synthesis by incorporating into DNA during the S phase of the cell cycle, leading to inhibition of DNA polymerase and repair mechanisms. The combination has been shown to have synergistic effects in CML, improving molecular response rates compared to monotherapy[1][2][3][5]. This regimen has been studied in phase II clinical trials for newly diagnosed CML patients.

02

Targets

ABL1 myristoyl pocketPDGFR (PDGFR family)KIT (c-KIT proto-oncogene receptor tyrosine kinase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)POLA1 (DNA polymerase alpha)POLB (DNA polymerase beta)

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