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temuterkib + midazolam
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
LY3214996 + midazolam is a drug-drug interaction (DDI) study combination used in clinical research. **LY3214996** (temuterkib) is a potent, selective, small-molecule ATP-competitive inhibitor of extracellular signal-regulated kinase 1 and 2 (ERK1/2), developed by Eli Lilly. It targets the MAPK/ERK signaling pathway, which is frequently dysregulated in cancers harboring BRAF or RAS mutations. **Midazolam** is a short-acting benzodiazepine that acts as a positive allosteric modulator of the GABA-A receptor. In the context of oncology clinical trials (such as NCT02857270), midazolam is utilized as a sensitive probe substrate for the cytochrome P450 3A4 (CYP3A4) enzyme. The combination is administered to evaluate the potential for LY3214996 to inhibit or induce CYP3A4 metabolism, thereby informing the safety profile and dosing requirements when temuterkib is co-administered with other medications metabolized by this pathway.
- Other names
- LY3214996 + midazolamtemuterkib + midazolam
02
Targets
BZD site (GABA-A receptor benzodiazepine site)MAPK3 (Mitogen-activated protein kinase 1)
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