LIB-01

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LIB-01
Clinical data
Other namesLIB01; DIC-2024; DIC2024; Libiguin
Routes of
administration 		Oral [1] [2]
Drug class Indirect melanocortin MC4 receptor potentiator

LIB-01, also known as DIC-2024 or as Libiguin, is an indirect melanocortin MC4 receptor potentiator which is under development for the treatment of erectile dysfunction and premature ejaculation. [1] [3] It is taken orally. [2]

Contents

The drug works by increasing expression of the melanocortin MC4 receptor and of its endogenous agonist in the brain. [3] [4] In relation to this, its mechanism of action differs from that of earlier direct melanocortin receptor agonists like bremelanotide. [2] [5] As such, the drug is described as a potential first-in-class medication. [2] [5] LIB-01 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. [3] [2] [5] [6] [7] The pro-erectile effects of LIB-01 can be reversed by a melanocortin MC4 receptor antagonist in rodents. [3] [4]

LIB-01 is a semisynthetic analogue of alkaloids from Neobeguea mahafalensis root bark such as libiguin A and libiguin B. [7] [8] Neobeguea mahafalensis has a long history of traditional use in Madagascar. [7] 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. [8] [9] This specifically included having very high potency and a remarkably long-lasting duration in increasing mounting behavior in male rodents. [8]

LIB-01 was originated by Uppsala University and is under development by Dicot Pharma. [1] As of December 2025, 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. [3] [4] The exact chemical structure of LIB-01 does not yet appear to have been disclosed. [1]

See also

References

  1. 1 2 3 4 5 "LIB 01". AdisInsight. 26 December 2025. Retrieved 27 January 2026.
  2. 1 2 3 4 5 Padma-Nathan H, Rosen R, Forest C, Holmberg M, Gauffin C (12 August 2024). "(129) Results of a First-In-Human Trial of Lib-01, A Novel, First in Class Potential Oral ed Drug with Unique Pharmacodynamic Properties". The Journal of Sexual Medicine. 21 (Supplement_7) qdae167.127. doi:10.1093/jsxmed/qdae167.127. ISSN   1743-6095 . Retrieved 27 January 2026.
  3. 1 2 3 4 5 Foster B (12 January 2026). "A new approach could radically change erectile dysfunction treatment". Drug Discovery News. Retrieved 27 January 2026.
  4. 1 2 3 "Dicot Pharma presents new research findings on the mechanism of action of LIB-01". Dicot Pharma. 7 December 2025.
  5. 1 2 3 Giuliano F, Padma-Nathan H, Rosen RC, Forest C, Holmberg M, Gauffin C (9 May 2025). "Early Clinical Development Program, Including Results of a First-In-Human Trial of Lib-01, A Novel, First in Class Potential Oral Erectile Dysfunction Drug with Unique Pharmacodynamic Properties". The Journal of Sexual Medicine. 22 (Supplement_2) qdaf077.083. doi:10.1093/jsxmed/qdaf077.083. ISSN   1743-6095 . Retrieved 27 January 2026.
  6. ↑ Giuliano F, Gorny D, Razanakolona M, Behr-Roussel D, Assaly R, Gauffin C (5 February 2024). "(370) Overview of Nonclinical Studies of LIB-01, a Novel Promising Oral Drug Under Development for Treatment of Erectile Dysfunction". The Journal of Sexual Medicine. 21 (Supplement_1) qdae001.355. doi:10.1093/jsxmed/qdae001.355. ISSN   1743-6095 . Retrieved 27 January 2026.
  7. 1 2 3 Razanakolona M, Bradesi C, Laurin M, Fugl-Meyer K, Behr-Roussel D, Giuliano F, et al. (1 November 2022). "Prolonged Pro-Erectile Facilitator Effect of Lib-01 in Anesthetized Wistar Rats". The Journal of Sexual Medicine. 19 (Supplement_4): S3. doi:10.1016/j.jsxm.2022.08.082. ISSN   1743-6109 . Retrieved 27 January 2026.
  8. 1 2 3 Razafimahefa S, Mutulis F, Mutule I, Liepinsh E, Dambrova M, Cirule H, et al. (March 2014). "Libiguins A and B: novel phragmalin limonoids isolated from Neobeguea mahafalensis causing profound enhancement of sexual activity". Planta Medica. 80 (4): 306–314. doi:10.1055/s-0033-1360390. PMID   24549927.
  9. ↑ Grigorjeva L, Liepinsh E, Razafimahefa S, Yahorau A, Yahorava S, Rasoanaivo P, et al. (May 2014). "Semisynthesis of libiguin A and its analogues by trans-lactonization of phragmalin". The Journal of Organic Chemistry. 79 (9): 4148–4153. doi:10.1021/jo500318w. PMID   24716657.
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