| Bioactivity | Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist. | ||||||||||||
| Target | NK3R | ||||||||||||
| Invitro | Pavinetant (AZD2624) is a potent and selective NK3 receptor antagonist which is developed for the treatment of schizophrenia. Pavinetant exhibits an inhibitory effect on microsomal CYP3A4/5 activities with apparent IC50 values of 7.1 and 19.8 μM for midazolam and testosterone assays, respectively. No time-dependent inactivation of CYP3A4/5 activity by Pavinetant is observed. Pavinetant demonstrates weak to no inhibition of CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, and CYP2D6[1]. | ||||||||||||
| Name | Pavinetant | ||||||||||||
| CAS | 941690-55-7 | ||||||||||||
| Formula | C26H25N3O3S | ||||||||||||
| Molar Mass | 459.56 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Li Y, et al. In vitro assessment of metabolic drug–drug interaction potential of AZD2624, neurokinin-3 receptor antagonist, through cytochrome P(450) enzyme identification, inhibition, and induction studies. Xenobiotica. 2010 Nov;40(11):721-9. |