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| Clinical data | |
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| Other names | CVL-354 |
| Routes of administration | Oral administration |
| Drug class | Opioid antagonist;κ-Opioid receptor antagonist |
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| Chemical and physical data | |
| Formula | C23H26N4O3 |
| Molar mass | 406.486 g·mol−1 |
| 3D model (JSmol) | |
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Icalcaprant[1] (developmental code nameCVL-354) is anopioid antagonist which is under development for the treatment ofmajor depressive disorder andsubstance-related disorders.[2][3] It is takenby mouth.[2]
It acts as aselectiveantagonist of theκ-opioid receptor.[2][3] The drug is also more weakly an antagonist of theμ-opioid receptor, with about 31-fold loweraffinity and 27-fold lower inhibitorypotency at the μ-opioid receptor relative to the κ-opioid receptor.[3]
It was originated byPfizer and is under development byCerevel Therapeutics (a subsidiary ofAbbVie).[2][4] As of September 2022, icalcaprant is inphase 1clinical trials for major depressive disorder and is in thepreclincal stage of development for substance-related disorders.[2]
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