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NKTR-118 + rifampin
- Development stage
- Unknown
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
NKTR-118 + rifampin is an experimental drug combination consisting of NKTR-118 (pegylated naloxol, a peripherally acting mu-opioid receptor antagonist) and rifampin (an antibiotic and potent cytochrome P450 inducer). NKTR-118 (naloxegol) was developed for the treatment of opioid-induced constipation (OIC) and is designed to block opioid receptors in the gut with minimal central nervous system penetration due to its PEGylation. Rifampin is included in this combination specifically to study its effects on the pharmacokinetics of NKTR-118, since rifampin is known to be a strong inducer of various drug-metabolizing enzymes and transporters. The combination itself is not used therapeutically but rather to characterize drug–drug interactions and metabolism in clinical pharmacology studies in healthy volunteers[1][5]. Nektar Therapeutics initially developed NKTR-118; AstraZeneca has developed and marketed naloxegol as Movantik.
- Brand names
- Movantik
- Other names
- naloxegolNKTR-118NKTR118NKTR 118rifampicin
02
Targets
RNAP (Bacterial dna-dependent RNA polymerase)ABCB1 (P-glycoprotein)UGT (UDP-glucuronosyltransferase family)CYP3A4 (Cytochrome P450 3A4)MOR (Mu opioid receptor)PXR (Pregnane X receptor)
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