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trantinterol
- Development stage
- Unknown
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Trantinterol is a novel, orally active small molecule that acts as a β2-adrenoceptor (β2-adrenergic receptor) agonist. It is primarily developed for the treatment of asthma and related respiratory conditions. In addition to its bronchodilatory effects via β2-adrenoceptor activation, trantinterol has been shown to be a potent noncompetitive inhibitor of P-glycoprotein (P-gp), which may increase the bioavailability of other drugs that are P-gp substrates when coadministered. Trantinterol undergoes extensive metabolism in the liver, mainly by cytochrome P450 enzymes CYP3A4 and CYP2C19, with minor contributions from CYP2D6 and CYP2E1[1][3][4][6].
- Other names
- trantinterol hydrochloride
02
Targets
ADRB2 (β2)ABCB1 (P-glycoprotein)
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