Drug intelligence / Profile preview

SKLB1028 + midazolam

Development stage
Phase 1
Lead developer
CSPC Ouyi Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

SKLB1028 + midazolam refers to the co-administration of **SKLB1028**, a novel multi-target oral small molecule protein kinase inhibitor (targeting FLT3, EGFR, ABL, and Lyn kinases), and **midazolam**, a well-established benzodiazepine used primarily for its sedative, anxiolytic, and anticonvulsant properties. SKLB1028 is primarily under development for the treatment of acute myeloid leukemia (AML) with FLT3-ITD mutations and is in late-stage clinical trials. Drug–drug interaction (DDI) studies with midazolam are performed to assess effects on CYP3A4 activity, as midazolam is a sensitive probe substrate for this enzyme, and SKLB1028 is known to be metabolized by CYP3A4. The combination is not developed as a fixed-dose therapy, but studied for pharmacokinetic interactions relevant to clinical safety and efficacy assessment in oncology drug development[1].

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)EGFR (Epidermal growth factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)LYN (LYN proto-oncogene, Src family tyrosine kinase)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)

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