Volufralin
Pharmaceutical compound
From Wikipedia, the free encyclopedia
Volufralin (INN;[3] developmental code names LIB-01, DIC-2024, and Libiguin) is an indirect melanocortin MC4 receptor potentiator which is under development for the treatment of erectile dysfunction and premature ejaculation.[1][4] It is taken orally.[2]
| |
| Clinical data | |
|---|---|
| Other names | LIB-01; LIB01; DIC-2024; DIC2024; Libiguin |
| Routes of administration | Oral[1][2] |
| Drug class | Indirect melanocortin MC4 receptor potentiator |
| Pharmacokinetic data | |
| Onset of action | 15–120 min (Tmax[2] |
| Elimination half-life | ≪12 hours[2] |
| Identifiers | |
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| CAS Number | |
| Chemical and physical data | |
| Formula | C33H40O12 |
| Molar mass | 628.671 g·mol−1 |
Pharmacology
Volufralin works by increasing expression of the melanocortin MC4 receptor and of its endogenous agonist in the brain.[4][5] In relation to this, its mechanism of action differs from that of earlier direct melanocortin receptor agonists like bremelanotide.[2][6] As such, the drug is described as a potential first-in-class medication.[2][6] Volufralin produces non-acute long-lasting pro-erectile effects in rodents and humans, with short-term dosing resulting in gradually increasing improvement that is then sustained for weeks despite cessation of dosing.[4][2][6][7][8] The pro-erectile effects of volufralin can be reversed by a melanocortin MC4 receptor antagonist in rodents.[4][5]
Chemistry
Volufralin is a semisynthetic analogue of limonoids from Neobeguea mahafalensis root bark such as libiguin A and libiguin B.[8][9] Neobeguea mahafalensis has a long history of traditional use in Madagascar.[8] In 2014, libiguin A and B were discovered via isolation from the roots of the plant and were found to cause "profound enhancement of sexual activity" in rodents.[9][10] This specifically included having very high potency and a remarkably long-lasting duration in increasing mounting behavior in male rodents.[9]
History
Volufralin was originated by Uppsala University in Sweden and is under development by Dicot Pharma.[1] As of July 2026, it is in phase 2 clinical trials for erectile dysfunction and the preclinical research stage of development for premature ejaculation.[1] The mechanism of action of the drug of indirect melanocortin MC4 receptor potentiation was not initially disclosed, but was announced by its developer in December 2025.[4][5] The exact chemical structure of volufralin was not initially disclosed, aside from it being related to the libiguins.[1][8][9] However, in July 2026, the generic name of volufralin and its structure were published.[3]