Drug intelligence / Profile preview

bosutinib + capecitabine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Bosutinib + capecitabine is an investigational oral combination therapy evaluated for the treatment of advanced solid tumors, including locally advanced or metastatic breast, pancreatic, and colorectal cancers, as well as cholangiocarcinoma and glioblastoma. Bosutinib is a competitive Src/Abl tyrosine kinase inhibitor that targets signaling pathways involved in tumor cell proliferation and survival. Capecitabine is an antimetabolite prodrug that is enzymatically converted to 5-fluorouracil (5-FU) within tumor cells, where it inhibits DNA synthesis and cell division. The combination was studied in a phase 1 trial to determine its maximum tolerated dose (MTD), safety profile, and preliminary efficacy. The MTD was established at bosutinib 300 mg once daily plus capecitabine 1000 mg/m² twice daily; the regimen demonstrated manageable toxicity with adverse events similar to those seen with each agent alone[1][2]. Limited clinical efficacy was observed in this early-phase study.

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)SFK (SRC family kinases)TS (Thymidylate synthase)

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