Rolapitant
Rolapitant is a selective and long-acting neurokinin 1 (NK1) receptor antagonist that blocks substance P binding to NK1 receptors in the central and peripheral nervous system, preventing delayed emesis triggered by chemotherapy-induced release of substance P in the gut and brainstem. It is approved as an antiemetic for prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic chemotherapy.
Молекулярная масса
500,5000 g/mol
LogP
4,40
TPSA
50,40 Ų
Правило пяти Липинского
Соответствует
Механизм действия
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
2D Структура
Cite this structure
Embed this structure
SMILES
C[C@@H](OC[C@@]1(c2ccccc2)CC[C@]2(CCC(=O)N2)CN1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1
InChI
InChI=1S/C25H26F6N2O2/c1-16(17-11-19(24(26,27)28)13-20(12-17)25(29,30)31)35-15-23(18-5-3-2-4-6-18)10-9-22(14-32-23)8-7-21(34)33-22/h2-6,11-13,16,32H,7-10,14-15H2,1H3,(H,33,34)/t16-,22-,23-/m1/s1
Molecular Formula
C25H26F6N2O2
HBD / HBA
2 / 9
Вращаемые Связи
5
Тяжёлые Атомы
35
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Часто задаваемые вопросы
Rolapitant is a selective and long-acting neurokinin 1 (NK1) receptor antagonist that blocks substance P binding to NK1 receptors in the central and peripheral nervous system, preventing delayed emesis triggered by chemotherapy-induced release of substance P in the gut and brainstem. It is approved as an antiemetic for prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic chemotherapy.
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Yes, Rolapitant is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL3707331. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 10311306. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
Медицинский отказ от ответственности
This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
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