Drug intelligence / Profile preview

bosutinib + aprepitant

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

Overview

Bosutinib is an oral, small molecule tyrosine kinase inhibitor (TKI) that targets BCR-ABL and Src-family kinases, used primarily for the treatment of Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML), including cases resistant or intolerant to prior therapy. It inhibits most imatinib-resistant BCR-ABL mutations except T315I and V299L[2][8]. Aprepitant is a selective high-affinity antagonist of the human substance P/neurokinin 1 (NK1) receptor, used in combination with other antiemetics to prevent acute and delayed nausea and vomiting associated with chemotherapy or surgery[5][6]. When coadministered, aprepitant—a moderate CYP3A4 inhibitor—increases bosutinib plasma concentrations by inhibiting its metabolism via CYP3A4[4]. This combination may be relevant in oncology settings where both drugs are indicated: bosutinib for CML treatment and aprepitant for prevention of chemotherapy-induced nausea.

Other names
bosutinib + aprepitant
02

Targets

CYP3A4 (Cytochrome P450 3A4)SFK (SRC family kinases)TACR1 (Neurokinin‑1 Receptor)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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