Bupropion/trazodone

Bupropion/trazodone
Combination of
BupropionNorepinephrine–dopamine reuptake inhibitor (NDRI), other actions
TrazodoneSerotonin antagonist and reuptake inhibitor (SARI), other actions
Clinical data
Other namesLorexys; Orexa; S1P-104; S1P-205; SIP-104; Trazodone/bupropion
Routes of
administration		Oral[1][2]

Bupropion/trazodone (developmental code names S1P-104 and S1P-205; proposed brand names Lorexys and Orexa) is a combination of the norepinephrine–dopamine reuptake inhibitor (NDRI) bupropion and the serotonin antagonist and reuptake inhibitor (SARI) trazodone which is under development for the treatment of erectile dysfunction, female sexual dysfunction, and male sexual dysfunction.[1][3][4][5][2] It is taken orally.[1][2] Both bupropion and trazodone have individually been found to be effective and used for treating sexual dysfunction, such as low sexual desire or erectile dysfunction.[6][7][8][9][10] Bupropion/trazodone is under development by S1 Pharmaceuticals or S1 Biopharma.[1] As of September 2021, it is in phase 2 clinical trials for erectile dysfunction and female sexual dysfunction, whereas no recent development has been reported for male sexual dysfunction.[1]

See also

References

  1. ^ a b c d e "Bupropion/trazodone". AdisInsight. 27 September 2021. Retrieved 27 January 2026.
  2. ^ a b c Pyke RE, Clayton AH (December 2019). "Dose-Finding Study of Lorexys for Hypoactive Sexual Desire Disorder in Premenopausal Women". The Journal of Sexual Medicine. 16 (12): 1885–1894. doi:10.1016/j.jsxm.2019.09.005. PMID 31678098.
  3. ^ Miller MK, Smith JR, Norman JJ, Clayton AH (September 2018). "Expert opinion on existing and developing drugs to treat female sexual dysfunction". Expert Opinion on Emerging Drugs. 23 (3): 223–230. doi:10.1080/14728214.2018.1527901. PMID 30251897. iii) Bupropion-trazodone combination (Lorexys) Bupropion, a norepinephrine-dopamine reuptake inhibitor (NDRI) and trazodone, a 5-HT1A partial agonist, 5-HT2A antagonist and α1 antagonist would theoretically enhance sexual excitation and diminish inhibition. In a crossover phase 2a study of HSDD in premenopausal women using two proprietary dose combinations of bupropion-trazodone (low and moderate) vs. bupropion 300 mg/d (control), moderate dose Lorexys demonstrated >30% superiority over control, with 76% vs. 38% response on FSFI desire score and 58% of women achieving remission of low desire (FSFI-D score >5) vs. 24% respectively. Distress/bother associated with low desire was also significantly decreased with moderate dose Lorexys vs. bupropion alone. Mean response occurred at 4 weeks, with the most common reported side effect of sedation, and of 26 subjects (3.8%) discontinuing due to clitoral swelling/priapism. [38] S1 Biopharma has a Phase IIb placebo-controlled study planned.
  4. ^ de Oliveira L, Vignozzi L, Giraldi A, Varod S, Corona G, Reisman Y (2024). "What Women Want? The State of the Art regarding the Treatment of Young Women with Hypoactive Sexual Desire Disorder". Pharmacology. 109 (2): 69–75. doi:10.1159/000535587. PMC 11006276. PMID 38151009. Lorexys® is a combination of the antidepressants bupropion (a dopamine/norepinephrine reuptake inhibitor) and trazodone (a serotonergic agonistantagonist), which are implicated in neurotransmission regulating sexual inhibition and exhibition [44, 45]. Initial trials with premenopausal women find a decrease in sexual distress and some adverse effects such as dry mouth, somnolence, headache, and dizziness [46].
  5. ^ How A, Jowdy C, Novatcheva E, Clayton AH (March 2025). "Novel Pharmacologic Treatments of Female Sexual Dysfunction". Clinical Obstetrics and Gynecology. 68 (1): 10–14. doi:10.1097/GRF.0000000000000922. PMID 39846877. Lorexys is an investigational drug combining bupropion (a dopamine-norepinephrine reuptake inhibitor) and trazodone (a serotonin agonist-antagonist) in a proprietary ratio. A Phase 2A trial demonstrated that Lorexys was superior to 150 mg/d bupropion alone, with good tolerability and adverse effects fitting the expected adverse effect profile of trazodone. On the basis of FSFI-D, 58% of patients receiving moderate dose Lorexys reached remission compared with 24% with bupropion alone (P< 0.05). Likewise, based on FSDS-R-13, 75% of patients receiving moderate dose Lorexys responded to treatment compared with 32% with bupropion alone.29
  6. ^ Goldstein I, Kim NN, Clayton AH, DeRogatis LR, Giraldi A, Parish SJ, et al. (January 2017). "Hypoactive Sexual Desire Disorder: International Society for the Study of Women's Sexual Health (ISSWSH) Expert Consensus Panel Review". Mayo Clinic Proceedings. 92 (1): 114–128. doi:10.1016/j.mayocp.2016.09.018. PMID 27916394.
  7. ^ Razali NA, Sidi H, Choy CL, Roos NA, Baharudin A, Das S (2022). "The Role of Bupropion in the Treatment of Women with Sexual Desire Disorder: A Systematic Review and Meta-Analysis". Current Neuropharmacology. 20 (10): 1941–1955. doi:10.2174/1570159X20666220222145735. PMC 9886814. PMID 35193485.
  8. ^ Pyke RE (April 2020). "Trazodone in Sexual Medicine: Underused and Overdosed?". Sexual Medicine Reviews. 8 (2): 206–216. doi:10.1016/j.sxmr.2018.08.003. PMID 30342856.
  9. ^ Fink HA, MacDonald R, Rutks IR, Wilt TJ (September 2003). "Trazodone for erectile dysfunction: a systematic review and meta-analysis". BJU International. 92 (4): 441–446. doi:10.1046/j.1464-410x.2003.04358.x. PMID 12930437.
  10. ^ Bossini L, Casolaro I, Koukouna D, Cecchini F, Fagiolini A (August 2012). "Off-label uses of trazodone: a review". Expert Opinion on Pharmacotherapy. 13 (12): 1707–1717. doi:10.1517/14656566.2012.699523. PMID 22712761.
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