Orenetide

Last updated

Orenetide
Orenetide.svg
Clinical data
Trade names Libicore (proposed), Desirix (proposed)
Other namesBP101; BP-101; Thr-Lys-Pro-Arg-Pro; L-threonyl-L-lysyl-L-prolyl-L-arginyl-L-proline; "Female Viagra"
Routes of
administration 		Intranasal (nasal spray) [1] [2] [3] [4]
Drug class Unknown [1] [2] [4]
Identifiers
  • (2S)-1-[(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carboxylic acid
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C26H47N9O7
Molar mass 597.718 g·mol−1
3D model (JSmol)
  • C[C@H]([C@@H](C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)O)N)O
  • InChI=1S/C26H47N9O7/c1-15(36)20(28)22(38)33-16(7-2-3-11-27)23(39)34-13-5-9-18(34)21(37)32-17(8-4-12-31-26(29)30)24(40)35-14-6-10-19(35)25(41)42/h15-20,36H,2-14,27-28H2,1H3,(H,32,37)(H,33,38)(H,41,42)(H4,29,30,31)/t15-,16+,17+,18+,19+,20+/m1/s1
  • Key:XHFIMNICAYXOAS-HLXURNFRSA-N

Orenetide (INN Tooltip International Nonproprietary Name; developmental code name BP101, proposed brand names Libicore and Desirix), also known as Thr-Lys-Pro-Arg-Pro or as so-called "female Viagra", is a synthetic small peptide drug which is under development for the treatment of female sexual dysfunction, or more specifically hypoactive sexual desire disorder (HSDD). [1] [5] [2] [6] [7] [4] [8] It is taken intranasally as a nasal spray. [1] [2] [3] [4]

Contents

The mechanism of action of orenetide has not been fully elucidated and is unknown. [1] [2] [4] It was inactive at a panel of 98  G protein-coupled receptors (GPCRs), including serotonin, dopamine, and melanocortin receptors, among others. [9] However, at high concentrations in vitro , it inhibited selected GABAA receptors, which may be involved in its effects. [4] [8] Relatedly, it has been labeled in some sources as a "GABAA receptor antagonist". [10] [5] The drug produces pro-sexual effects in rodents, with these effects appearing to be mediated in the medial preoptic area. [6] [4] [9] It is described as a potential first-in-class medication. [7]

The drug was originated by Ivix and is under development by Ovoca Bio. [1] [5] [2] As of January 2021, it is in the preregistration phase of development. [1] [5] [2] In August 2023, it was announced that orenetide had failed to show efficacy for sexual desire or sexual distress in a large dose-ranging phase 2 clinical trial for treatment of HSDD. [3] [11] Shares of Ovoca Bio fell by as much as 82% following the announcement. [3] [11] Ovoca Bio is Ireland-based and orenetide has been developed in Australia, New Zealand, and Russia. [8] [11] [4] It reached phase 2 trials in Australia and New Zealand and completed phase 3 trials in Russia and was submitted for marketing approval in that country. [8] [12]

See also

References

  1. 1 2 3 4 5 6 7 "BP 101 - Ovoca Bio". AdisInsight. 8 January 2021. Retrieved 27 January 2026.
  2. 1 2 3 4 5 6 7 "Orenetide Drug Profile". Ozmosi. 1 January 1900. Retrieved 27 January 2026.
  3. 1 2 3 4 Dennis M (31 August 2023). "Ovoca Bio implodes on study failure of drug for female sexual desire disorder". firstwordpharma.com. Retrieved 27 January 2026.
  4. 1 2 3 4 5 6 7 8 Sukhikh SG, Smulevich SA, Stenyaeva SN, Nemenov D ND, Prilepskaya PV, Khritinin KD, et al. (30 August 2022). "Orenetide for the treatment of hypoactive sexual desire disorder: results of a randomized placebo-controlled trial". Akusherstvo I Ginekologiia. 8_2022: 95–106. doi:10.18565/aig.2022.8.95-106. ISSN   2412-5679 . Retrieved 27 January 2026. Desirix (INN orenetide, code name BP101) is an investigational drug consisting of a five amino acid peptide, intended for bilateral intranasal spray application. The mechanism of action of Desirix is currently not fully elucidated, but there is evidence to indicate it works by acting on the brain structures responsible for the regulation of sexual and reproductive behavior [10]. Intranasal administration of Desirix stimulated sexual behavior in rats, most likely by acting on the nuclei of the hypothalamus and limbic-reticular system [10]. It has been shown that Desirix is delivered to the site of activity via the nasal mucosa to the neurons of the olfactory bulbs and then through their axons that comprise the olfactory tracts on the basal surface of the brain, into the hypothalamic structures. In vitro Desirix at high concentrations inhibits the activation of selected gamma-amino butyric acid (GABA)A receptors. These data are aligned with the established notion that GABA affects sexual behavior [11–14]. Additionally, Desirix stimulates sexual behavior in animals when injected intracranially into the preoptic area, an area with demonstrated roles in reproduction and sexual behavior [10, 15–17]. Recent data suggest that Desirix affects the mechanisms of glutamate neuronal transmission in the diencephalon and possibly in the prefrontal cortex.
  5. 1 2 3 4 "Delving into the Latest Updates on BP-101(Ovoca Bio) with Synapse". Synapse. 10 January 2026. Retrieved 27 January 2026.
  6. 1 2 Both S (2017). "Recent Developments in Psychopharmaceutical Approaches to Treating Female Sexual Interest and Arousal Disorder". Current Sexual Health Reports. 9 (4): 192–199. doi:10.1007/s11930-017-0124-3. PMC   5711968 . PMID   29225554. BP101 Another new drug under investigation is BP101, a synthetic peptide molecule. The structure has not been disclosed for commercial reasons. The effect of the drug on sexual behavior was tested in three experiments in female rats [35], one experiment on the acute effects of a single intranasal administration, one on the effects of long-term (16 days) daily intranasal administration, and one on the effects of administration directly into the brain, more specifically into the olfactory bulb, the ventral medial hypothalamus, the MPOA, or the ventral tegmental area. Effects on solicitation, lordosis, and social approach behaviors, as well as genital sniffing, were studied. In experiments 1 and 2, an effect of BP101 was observed for solicitation behavior only. In experiment 3, it was observed that administration of BP101 in the MPOA and not in other brain areas increased solicitation behaviors. BP101 is currently undergoing randomized, double-blinded, placebo-controlled phase II studies. Safety, tolerability, pharmacokinetics, pharmacodynamics, and effects on sexual function will be studied after multiple-dose administration of BP101 nasal spray in healthy volunteers [...] and in women with HSDD [...].
  7. 1 2 Nappi RE, Tiranini L, Cucinella L, Martini E, Bosoni D, Righi A, et al. (January 2023). "Pharmacotherapy for female sexual dysfunctions (FSDs): what is on the market and where is this field heading?". Expert Opinion on Pharmacotherapy. 24 (1): 135–143. doi:10.1080/14656566.2022.2066997. PMID   35430926. Ovoca Bio (Dublin, Ireland) is currently developing Orenetide (BP-101), a novel synthetic peptide, as a potential nasal spray for first-in-class treatment to stimulate sexual motivation [88]. Experimental placebo-controlled data showed that acute intranasal BP101 administration moderately increased the frequency of solicitations, an indicator of sexual motivation in female rats, by acting within the hypothalamus under different hormonal conditions [93]. A Phase 2, multicenter, double-blind, randomized, placebo-controlled trial is ongoing in New Zealand and Australia to demonstrate the efficacy and safety of different doses of BP101 in premenopausal women with HSDD [89].
  8. 1 2 3 4 Dutton G (9 August 2021). "Ovoca Bio's "Female Viagra" Nasal Spray Inching Closer to Market". BioSpace. Retrieved 27 January 2026.
  9. 1 2 Andreev-Andrievskiy A, Lomonosov M, Popova A, Lagereva E, Clément P, Salimov R, et al. (March 2017). "BP101 Peptide Promotes Female Sexual Receptivity in the Rat". The Journal of Sexual Medicine. 14 (3): 336–346. doi:10.1016/j.jsxm.2017.01.008. PMID   28189563. To elucidate the mechanism of action, BP101 was screened on a panel of 98 G-proteinecoupled receptor characteristic for the brain. Screening was conducted by the DiscoveRx Corporation (Fremont, CA, USA). Among others, the panel contained serotonin, dopamine, and melanocortin receptors. BP101 was tested as an agonist, antagonist, and positive allosteric modulator. No change in activity was observed for any combination of the receptor and experimental mode.
  10. ↑ "Proposed INN: List 125" (PDF). WHO Drug Information. 35 (2). 2021. Prenetidum orenetide L-threonyl-L-lysyl-L-prolyl-L-arginyl-L-proline GABAA receptor antagonist
  11. 1 2 3 "Ovoca Bio shares plummet as female libido treatment trial fails". The Pharmaletter. 1 September 2023. Retrieved 27 January 2026.
  12. ↑ Nemenov D, Lomonosov M, Golikov D (1 February 2018). "150 BP101 New Molecule for HSDD Treatment - Results of Proof-of-concept Phase 2a Study". The Journal of Sexual Medicine. 15 (Supplement_1): S41–S42. doi:10.1016/j.jsxm.2017.11.108. ISSN   1743-6109 . Retrieved 27 January 2026.
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