Chemistry:LIB-01

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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][2] It is taken orally.[3]

The drug works by increasing expression of the melanocortin MC4 receptor and of its endogenous agonist in the brain.[2][4] In relation to this, its mechanism of action differs from that of earlier direct melanocortin receptor agonists like bremelanotide.[3][5] As such, the drug is described as a potential first-in-class medication.[3][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.[2][3][5][6][7] The pro-erectile effects of LIB-01 can be reversed by a melanocortin MC4 receptor antagonist in rodents.[2][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.[2][4] The exact chemical structure of LIB-01 does not yet appear to have been disclosed.[1]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 "LIB 01". 26 December 2025. https://adisinsight.springer.com/drugs/800047257. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "A new approach could radically change erectile dysfunction treatment". 12 January 2026. https://www.drugdiscoverynews.com/a-new-approach-could-radically-change-erectile-dysfunction-treatment-16910. 
  3. ↑ 3.0 3.1 3.2 3.3 "(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). 12 August 2024. doi:10.1093/jsxmed/qdae167.127. ISSN 1743-6095. https://academic.oup.com/jsm/article/doi/10.1093/jsxmed/qdae167.127/7918991. Retrieved 27 January 2026. 
  4. ↑ 4.0 4.1 4.2 "Dicot Pharma presents new research findings on the mechanism of action of LIB-01". 7 December 2025. https://www.dicotpharma.com/en/press/press-releases/?slug=dicot-pharma-presents-new-research-findings-on-the-mechanism-of-action-of-lib-01. 
  5. ↑ 5.0 5.1 5.2 "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). 9 May 2025. doi:10.1093/jsxmed/qdaf077.083. ISSN 1743-6095. https://academic.oup.com/jsm/article/doi/10.1093/jsxmed/qdaf077.083/8127529. Retrieved 27 January 2026. 
  6. ↑ "(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). 5 February 2024. doi:10.1093/jsxmed/qdae001.355. ISSN 1743-6095. https://academic.oup.com/jsm/article/doi/10.1093/jsxmed/qdae001.355/7600787. Retrieved 27 January 2026. 
  7. ↑ 7.0 7.1 7.2 "Prolonged Pro-Erectile Facilitator Effect of Lib-01 in Anesthetized Wistar Rats.". The Journal of Sexual Medicine 19 (Supplement_4): S3. 1 November 2022. doi:10.1016/j.jsxm.2022.08.082. ISSN 1743-6109. https://academic.oup.com/jsm/article/19/Supplement_4/S3/7464619. Retrieved 27 January 2026. 
  8. ↑ 8.0 8.1 8.2 "Libiguins A and B: novel phragmalin limonoids isolated from Neobeguea mahafalensis causing profound enhancement of sexual activity". Planta Medica 80 (4): 306–314. March 2014. doi:10.1055/s-0033-1360390. PMID 24549927. Bibcode: 2014PlMed..80..306R. 
  9. ↑ "Semisynthesis of libiguin A and its analogues by trans-lactonization of phragmalin". The Journal of Organic Chemistry 79 (9): 4148–4153. May 2014. doi:10.1021/jo500318w. PMID 24716657. 

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