Molfile
Inchi
Smiles
Synonyms:
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rolapitant
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rolapitant hydrochloride
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varubi
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SCH619734
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SCH 619734
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An orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life.
- Molecular weight: 500.49
- Formula: C25H26F6N2O2
- CLOGP: 4.71
- LIPINSKI: 1
- HAC: 4
- HDO: 2
- TPSA: 50.36
- ALOGS: -5.48
- ROTB: 7
- Status: ONP
Legend: OFP - off patent OFM - off market ONP - on patent
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