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rosuvastatin + fexofenadine
- Development stage
- Unknown
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
"Arm 3 probes" refers to a specific combination of diagnostic probe substrates—rosuvastatin and fexofenadine—utilized in the third arm of a Phase 1 clinical trial (NCT03037931) sponsored by Celgene (a Bristol Myers Squibb company). This study was designed to evaluate the drug-drug interaction (DDI) potential of enasidenib (IDHIFA), an IDH2 inhibitor, in patients with IDH2-mutated acute myeloid leukemia (AML). In this context, rosuvastatin serves as a phenotypic probe for the Breast Cancer Resistance Protein (BCRP) and Organic Anion Transporting Polypeptides (OATP1B1 and OATP1B3), while fexofenadine serves as a probe for P-glycoprotein (P-gp). By measuring the pharmacokinetic changes of these substrates when co-administered with enasidenib at steady state, researchers can determine the inhibitory or inductive effects of enasidenib on these specific drug transporters.
- Brand names
- CrestorAllegra
- Other names
- arm 3 probesarm3 probesarm-3 probesrosuvastatin and fexofenadine
02
Targets
HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)HRH1 (Histamine H1 Receptor)SLCO1B3 (Organic anion transporting polypeptide 1B3)ABCB1 (P-glycoprotein)OATP1B1 (Organic anion transporting polypeptide 1B1)ABCG2 (Breast cancer resistance protein)
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