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osimertinib + rosuvastatin
- Development stage
- Phase 1
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This is a combination of two medications: osimertinib (Tagrisso) and rosuvastatin (Crestor). Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor used for treating non-small cell lung cancer (NSCLC) with specific EGFR mutations. Rosuvastatin is a statin medication used to lower cholesterol levels. When co-administered, osimertinib has been shown to increase rosuvastatin exposure by approximately 35% due to osimertinib's inhibitory effect on breast cancer resistance protein (BCRP) transporter, of which rosuvastatin is a substrate.
- Brand names
- Tagrisso + Crestor
02
Targets
TNK2 (Activated Cdc42-associated kinase 1)ABCG2 (Breast cancer resistance protein)BLK (B lymphoid tyrosine kinase)EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB3 (Erb-b2 receptor tyrosine kinase 3)ERBB4 (Erb-b2 receptor tyrosine kinase 4)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)
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