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Drug intelligence / Profile preview
GDC-0032 + midazolam
- Development stage
- Discontinued
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral (GDC-0032), Oral (midazolam, In Studies)
01
Overview
**GDC-0032 + midazolam** is an experimental pharmacological combination used primarily in drug-drug interaction clinical studies to characterize the impact of taselisib (GDC-0032), a selective phosphatidylinositol 3-kinase (PI3K) inhibitor, on the pharmacokinetics of midazolam, a well-known substrate of cytochrome P450 3A4 (CYP3A4). Taselisib is orally bioavailable and selectively inhibits the alpha isoform of PI3K, showing increased efficacy in tumors with *PIK3CA* mutations, and is being developed mainly for oncology indications. Midazolam is a short-acting benzodiazepine commonly used as a probe drug for CYP3A4 activity in metabolic interaction studies, and is not intended as an oncologic therapy in this combination. The combination is not meant for therapeutic synergy but for assessing safety and metabolic interactions in the context of cancer drug development[1][3].
- Other names
- taselisib + midazolam
02
Targets
GABRR (GABA-A receptor subunit rho)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)PIK3CA (Phosphoinositide 3-kinase alpha)
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