List of investigational sexual dysfunction drugs

Preregistration

• Orenetide (BP-101; BP101; Libicore; Desirix) – undefined mechanism of action (synthetic small peptide) – female sexual dysfunction ^[1][2][3][4]
• Tadalafil oral film (AQST-119; Exordia) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Tadalafil oral film (Exordia; INT-007; INT0007; INT0007/2006) – phosphodiesterase PDE5 inhibitor – erectile dysfunction

Phase 3

• Clomipramine/sildenafil (CDFR-0812) – combination of clomipramine (tricyclic antidepressant (TCA), serotonin–norepinephrine reuptake inhibitor (SNRI), other actions) and sildenafil (phosphodiesterase PDE5 inhibitor) – premature ejaculation
• Gepirone (Ariza; BMY-13805-1; BMY-13805; Exxua; Gepirone ER; MJ-13805; Org-33062; TGFK07AD; Travivo; Variza) – serotonin 5-HT_1A receptor agonist, other actions – decreased libido
• Nitroglycerin gel (Eroxon; glyceryl trinitrate topical gel; MED-2001; MED-2003; MED-2004; MED-2005; MED-3000; MED2002) – guanylate cyclase stimulant, nitric oxide donor, nitric oxide stimulant – erectile dysfunction
• Prasterone vaginal (dehydroepiandrosterone; DHEA; Intrarosa; Vaginorm) – androgen (androgen receptor agonist), other actions – decreased libido
• Sacubitril/valsartan (AHU-377/valsartan; Enrest; Enresuto; Entresto; Entresto Sprinkle; LCZ-696; LCZ-696A; Neparvis; valsartan/AHU-377; valsartan/sacubitril) – combination of sacubitril (neprilysin inhibitor) and valsartan (angiotensin II receptor type 1 (AT₁) antagonist) – erectile dysfunction

Phase 2

• Aildenafil (methisosildenafil) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• AN-788 (IP-2018; IP2018; NSD788; NSD-788) – serotonin–dopamine reuptake inhibitor (SDRI) – erectile dysfunction
• Apomorphine intranasal (AL-101; intranasal apomorphine) – non-selective dopamine receptor agonist, other actions – erectile dysfunction, female sexual dysfunction
• Autologous mesenchymal stem cell therapy (autologous bone marrow-derived mesenchymal stem cell therapy; Cellgram; Cellgram-ED; Cellgram-LC; Cerecellgram-spine; Hearticellgram-AMI; Immunocellgram; Impocellgram; Livercellgram; Lungcellgram; MSC-1; MSC-2) – cell replacement – erectile dysfunction
• Botulinum toxin A (AboBoNT-A; AbobotulinumtoxinA; Alluzience; Azzalure; BoNT-A; BTX-A-HAC; BTX-A-HAC NG; Clostridium botulinum toxin type A haemagglutinin complex; Dysport; Dysport NG; Dysport RU; Dysport Solution; Dysport Next Generation; Reloxin) – acetylcholine release inhibitor and neuromuscular blocking agent – vulvodynia
• Bupropion/trazodone (Lorexys; Orexa; S1P-104; S1P-205; SIP-104; trazodone/bupropion) – combination of bupropion (norepinephrine–dopamine reuptake inhibitor (NDRI), other actions) and trazodone (serotonin antagonist and reuptake inhibitor (SARI), various actions) – erectile dysfunction, female sexual dysfunction, male sexual dysfunction
• Buspirone/testosterone (Lybridos; testosterone/buspirone) – combination of buspirone (serotonin 5-HT_1A receptor agonist, other actions) and testosterone (androgen) – female sexual dysfunction
• BZ-371A (PnPP-19) – nitric oxide stimulant – erectile dysfunction, female sexual dysfunction
• Cligosiban (IX-01; PF-3274167) – oxytocin receptor antagonist – premature ejaculation
• Estetrol (Donesta; E4) – estrogen (estrogen receptor agonist) – atrophic vaginitis, female sexual dysfunction
• Estriol vaginal ring (VR-102; VR102; long-acting estriol vaginal ring) – estrogen (estrogen receptor agonist) – atrophic vaginitis
• Fadanafil (XZP-5849) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• FKW-00GA (FKW00GA; TGW-00AA; TGW00AA; TGWOOAA; TGW-OOAA) – serotonin 5-HT_1A receptor agonist, serotonin 5-HT_2A receptor antagonist – sexual function disorders
• LIB-01 (DIC-2024; DIC2024; Libiguin) – indirect melanocortin MC₄ receptor potentiator – erectile dysfunction, premature ejaculation
• Onabotulinum toxin A (BoNTA; Botox; botulinum toxin A injectable; GSK-1358820; GSK1358820; OnabotA X; OnabotulinumtoxinA X; Vistabel; Vistabex) – acetylcholine release inhibitor and neuromuscular blocking agent – premature ejaculation
• OPK-88004 (LY-2452473; TT701) – selective androgen receptor modulator (SARM) – erectile dysfunction
• Pudafensine (IP2015; IP-2015) – serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) – erectile dysfunction, vulvodynia, female sexual dysfunction
• Sildenafil/testosterone (Lybrido; testosterone/sildenafil) – combination of sildenafil (phosphodiesterase PDE5 inhibitor) and testosterone (androgen) – female sexual dysfunction
• Sildenafil topical – phosphodiesterase PDE5 inhibitor – female sexual dysfunction
• Testosterone intranasal (low-dose) (MPP-14; Noseafix; TBS-2; Tefina) – androgen (androgen receptor agonist) – anorgasmia, decreased libido
• TGFK-09SD (TGFK09SD) – serotonin 5-HT_1A receptor agonist – female sexual dysfunction

Phase 1/2

• Mirabegron (Betanis; Betmiga; Betmiga PR; Myrbetriq; Myrbetriq Granules; YM-178) – β₃-adrenergic receptor agonist – erectile dysfunction

Phase 1

• KH-001 (KH001) – atypical selective serotonin reuptake inhibitor (SSRI), phosphodiesterase (PDE) inhibitor (purified Sceletium tortuosum (kanna) alkaloid; possibly mesembrine) – premature ejaculation ^[5][6][7]
• VV-913 (VV913) – undefined mechanism of action – premature ejaculation

Clinical phase unknown

• Sildenafil orally-dissolving film (NAL8238; NAL-8238; sildenafil ODF) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Tadalafil orally-dissolving film (NAL8233; NAL-8233; tadalafil ODF) – phosphodiesterase PDE5 inhibitor – erectile dysfunction

Preclinical

• CF-602 – adenosine A₃ receptor modulator – erectile dysfunction
• S1B-307 – "central nervous system modulator" – anorgasmia, female sexual dysfunction
• S1B-408 – undefined mechanism of action – anorgasmia
• S1B-3006 (S1B0-3006; S1B3006) – "central nervous system modulator" – sexual function disorders

Phase unknown

• Pirenzepine topical (topical pirenzepine; WST-057; WST-1; WST01; WST1/analgesic; WST57) – muscarinic acetylcholine M₁ receptor antagonist – sexual function disorders

No development reported

• AB-101 (RJ-101) – undefined mechanism of action – female sexual dysfunction
• Apomorphine intranasal – non-selective dopamine receptor agonist, other actions – erectile dysfunction, female sexual dysfunction
• Armodafinil ((R)-modafinil; D-modafinil; NH-02D; NH02D) – atypical dopamine reuptake inhibitor (DRI) – premature ejaculation ^[8]
• Deuterated testosterone (d3-testosterone) – androgen (androgen receptor agonist) – female sexual dysfunction
• Epelsiban (GSK557296; GSK-557296) – oxytocin receptor antagonist – premature ejaculation
• Estradiol/testosterone topical gel (LibiGel-E/T; testosterone/estradiol topical gel) – combination of estradiol (estrogen) and testosterone (androgen) – female sexual dysfunction
• Fibroblast growth factor 1 (FGF-1; FGF1; Acidic FGF; aFGF; Cardio Vascu-Grow; CVBT-141P; CVBT-141S; CVBT-141A; CVBT-141B; CVBT-141C; CVBT-141D; CVBT-141E; CVBT-141ED; CVBT-141F; CVBT-141G; CVBT-141H; FGF-1(141); VT-141D; VT-141ED; VT-141P; VT-141S) – fibroblast growth factor receptor (FGFR) agonist – erectile dysfunction
• FKK-01PD (FKK-01PD; TGHW-01AP; TGHW01AP) – non-selective dopamine receptor agonist, other actions (apomorphine prodrug) – erectile dysfunction
• GSK-958108 (GSK958108) – serotonin 5-HT_1A receptor antagonist – premature ejaculation
• HCP-1302 (HCP1302) – undefined mechanism of action – erectile dysfunction
• Lidocaine topical gel – sodium channel blocker, local anesthetic – dyspareunia
• PTL-2015 – undefined mechanism of action – erectile dysfunction
• Research programme: nerve-targeted gene therapy - Periphagen (NC-3; NE-2; NE2-Endomorphin; NG-2; NG2-GAD; NN1-Neurotrophin) – various actions – erectile dysfunction
• Research programme: sexual dysfunction therapy - Palatin Technologies (PL-6983) – melanocortin receptor modulators – erectile dysfunction, female sexual dysfunction
• Sildenafil (KW-25084) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Sildenafil orally soluble film (CURE-5003; CUREfilm Blue) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Sildenafil oral spray (Duromist; NVD-401; SUD-003; SUD-004; SUDA-004; Sudamist) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Tadalafil dry powder inhalation (Tadalafil Technosphere) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Tadalafil orodispersible film tablet (Caliberi) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Tadalafil topical (Extrinsa) – phosphodiesterase PDE5 inhibitor – female sexual dysfunction
• Tadalafil/tamsulosin – combination of tadalafil (phosphodiesterase PDE5 inhibitor) and tamsulosin (α₁-adrenergic receptor antagonist) – erectile dysfunction
• Tunodafil (ecocarbamate; gluconocin; yonkenafil) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Vilazodone (EMD-68843; SB-659746A; Viibryd) – serotonin reuptake inhibitor (SRI), serotonin 5-HT_1A receptor agonist – sexual function disorders
• Zotarolimus (ABT-578; Endeavor; Endeavor Resolute; MDT-4107 DES; Resolute DES; Resolute Integrity; Resolute Onyx; ZoMaxx) – FK-binding protein 12 (FKBP12) ligand and mechanistic target of rapamycin (mTOR) inhibitor – erectile dysfunction

Preregistration submission withdrawal

• Lasofoxifene (AZU-101; CP-336156; CP-336156-CB; Fablyn; HLX-78; Oporia) – selective estrogen receptor modulator (SERM) – atrophic vaginitis

Suspended

• Alprostadil topical (Alprox-TD; Befar; Cold Chain Vitaros; Femprox; RayVa; Room Temperature Vitaros; Virirec; Vitaros; Vytaros; WC-3036) – prostaglandin E1 (PGE1) agonist – female sexual dysfunction

Discontinued

• Acolbifene/prasterone (dehydroepiandrosterone/acolbifene; DHEA/acolbifene; prasterone/acolbifene; Femivia) – combination of acolbifene (selective estrogen receptor modulator (SERM)) and prasterone (dehydroepiandrosterone; DHEA) (androgen, other actions) – decreased libido
• Alprostadil SEPA (prostaglandin E1 SEPA; alprostadil/soft enhancement of percutaneous absorption; Topiglan) – prostaglandin E1 (PGE1) agonist – erectile dysfunction
• Alprostadil/lidocaine (NM02216; NM100061) – combination of alprostadil (prostaglandin E1 (PGE1) agonist) and lidocaine (sodium channel blocker, local anesthetic) – premature ejaculation
• Amesergide (LY-237733; LY237733; LY-237,733) – serotonin 5-HT_2A, 5-HT_2B, and 5-HT_2C receptor antagonist, other actions – erectile dysfunction, premature ejaculation
• Apomorphine inhalation (VR-004; VR-040; VR-400) – non-selective dopamine receptor agonist, other actions – erectile dysfunction, female sexual dysfunction
• Apomorphine intranasal – non-selective dopamine receptor agonist, other actions – erectile dysfunction
• Avanafil (Razatus; Spedra; Stendra; TA-1790; Zepeed) – phosphodiesterase PDE5 inhibitor – female sexual dysfunction, premature ejaculation
• BAY-604552 (BAY98-7081; sGC activator) – guanylate cyclase stimulant – erectile dysfunction
• Bremelanotide (Rekynda; Vyleesi; PT-141) – melanocortin MC₄ receptor agonist – erectile dysfunction
• CP-866087 (CP-866,087) – μ-opioid receptor antagonist – female sexual dysfunction
• DA-8031 (DA8031) – selective serotonin reuptake inhibitor (SSRI) – premature ejaculation
• Dapoxetine (IMD dapoxetine; YHD-1044) – selective serotonin reuptake inhibitor (SSRI) – premature ejaculation
• Delequamine (RS-15385; RS-15385197) – α₂-adrenergic receptor antagonist – erectile dysfunction
• Estradiol/testosterone transdermal (testosterone/estradiol transdermal) – combination of estradiol (estrogen) and testosterone (androgen) – female sexual dysfunction
• GM-1485 (GPI-1485; NIL-A) – immunophilin modulator – erectile dysfunction
• Heparin/lidocaine/sodium bicarbonate (alkalised lidocaine and heparin formulation; Hep-Lido-A compounded formulation; U-101; URG-101) – combination of heparin (Factor Xa inhibitor, thrombin inhibitor), lidocaine (sodium channel blocker, local anesthetic), and sodium bicarbonate (absorption enhancer) – dyspareunia
• hMaxi-K gene therapy (pVAX/hSlo; URO-902) – gene transference – erectile dysfunction
• INO-1001 (INO1001; Pardex) – poly(ADP-ribose) polymerase inhibitor – erectile dysfunction
• LGD-2941 (LGD2941; LGD122941; LGD-122941) – selective androgen receptor modulator (SARM) – female sexual dysfunction, male sexual dysfunction
• Melanotan II (MT-II; PT-14) – melanocortin receptor agonist – erectile dysfunction, male sexual dysfunction
• Milnacipran (Dalcipran; F-2207; Impulsor; Ixel; Joncia; Midacipran; Midalcipran; Savella; TN-912; Toledomin) – serotonin–norepinephrine reuptake inhibitor (SNRI) – vulvodynia
• Nitroglycerin topical (Anogesic; Cellegesic; Rectiv; Rectogesic) – nitric oxide donor – dyspareunia, vulvodynia
• NMI-870 – α₂-adrenergic receptor antagonist, nitric oxide donor – erectile dysfunction, female sexual dysfunction
• Oxytocin (oxytocin gel; oxytocin topical; Vagitocin) – oxytocin receptor agonist – atrophic vaginitis
• Pagoclone (IP-456; Panex; RP-62955) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/cyclopyrrolone – premature ejaculation
• PF-446687 (PF-00446687; PF-446,687) – melanocortin MC₄ receptor agonist – sexual function disorders
• PF-592379 (PF-000592379; PF-592,379) – dopamine D₃ receptor agonist – erectile dysfunction
• Research programme: therapeutics - Re-Pharm (RP-0217; RP0217) – protein phosphatase 2A (PP2A) inhibitor – sexual function disorders
• RO-0282425 (RO0282425) – melanocortin MC₄ receptor agonist – erectile dysfunction
• RTN-001 (KD-027; SLX-2101; SLx-2101) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• SAR-407899 (SAR407899; SAR407899A) – Rho-associated kinase inhibitor – erectile dysfunction
• Sertraline (Aremis; Besitran; CP-51974; CP-51974-01; Gladem; J Zoloft; Lustral; Serad; Serlain; Tatig; Zoloft) – selective serotonin reuptake inhibitor (SSRI) – premature ejaculation
• Sildenafil (Revatio; Revatio IV; UK-92480; Viagra) – phosphodiesterase PDE5 inhibitor – female sexual dysfunction
• Tadalafil (Adcirca; Cialis; GF-196960; IC-351; LY-450190; Zalutia) – phosphodiesterase PDE5 inhibitor – female sexual dysfunction
• Tadalafil sublingual (APC-8000) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Tadalafil/tamsulosin (CKD-397; tamsulosin/tadalafil) – combination of tadalafil (phosphodiesterase PDE5 inhibitor) and tamsulosin (α₁-adrenergic receptor antagonist) – erectile dysfunction
• Tadalafil/tamsulosin (YBH-1603) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• Testosterone topical (ESP-210) – androgen (androgen receptor agonist) – female sexual dysfunction
• Testosterone transdermal (FemTestosterone TDS) – androgen (androgen receptor agonist) – female sexual dysfunction
• Testosterone transdermal (Luramist; testosterone MDTS; testosterone transdermal spray) – androgen (androgen receptor agonist) – female sexual dysfunction
• TEMPE (Topical Eutectic Mixture for Premature Ejaculation) – undefined mechanism of action – premature ejaculation
• UK-357903 (UK-357,903) – phosphodiesterase PDE5 inhibitor – erectile dysfunction
• UK-390957 (UK-390,957) – serotonin reuptake inhibitor (SRI) – premature ejaculation
• UK-447841 (UK-447,841) – neprilysin inhibitor – female sexual dysfunction
• VML-670 (VML670; CEB-1555) – serotonin 5-HT_1A receptor agonist – female sexual dysfunction, male sexual dysfunction

Approved drugs

Market withdrawal

• Conjugated estrogens oral (Cenestin; synthetic conjugated estrogens) – estrogen (estrogen receptor agonist) – atrophic vaginitis
• Testosterone transdermal (Intrinsa; Intrinsa CHF; Livensa; Testosterone transdermal TheraDerm MTX; WC3048; WC3049) – androgen (androgen receptor agonist) – female sexual dysfunction

Off-label drugs

• α₂-Adrenergic receptor antagonists (e.g., yohimbine, rauwolscine (found in yohimbe)) – erectile dysfunction, low sexual desire ^{[18][19][20][21]}
• Androgens/anabolic steroids (androgen receptor agonists) (e.g., testosterone, testosterone esters, methyltestosterone) – low sexual desire ^[22]
• Antiandrogens (e.g., GnRH modulators, high-dose estrogen therapy, high-dose progestogen therapy) – various mechanisms of action – paraphilias, hypersexuality, sexual deviance^{[23][24][25][26]}
• Antipsychotics (e.g., haloperidol) – dopamine receptor antagonists, other actions – paraphilias, hypersexuality, sexual deviance ^[26]
• Bupropion (Wellbutrin, Zyban) – norepinephrine–dopamine reuptake inhibitor (NDRI), other actions – low sexual desire ^{[27][28][29][30][31]}
• Buspirone (Buspar) – serotonin 5-HT_1A receptor agonist, other actions – low sexual desire ^[27]
• Clomipramine (Anafranil) – tricyclic antidepressant (TCA), serotonin–norepinephrine reuptake inhibitor (SNRI), other actions – premature ejaculation ^[32][33]
• Cyproheptadine (Periactin) – non-selective serotonin receptor antagonist, other actions – anorgasmia, low sexual desire/decreased libido ^[34][35][36]
• Estrogens (e.g., estradiol, estradiol esters, ethinylestradiol) – estrogens (estrogen receptor agonists) – atrophic vaginitis, dyspareunia, vulvodynia, low sexual desire ^{[37][38][22][39]}
• Horny goat weed (Epimedii herba) – unknown mechanism of action – low sexual desire ^[19]
• Selective serotonin reuptake inhibitors (SSRIs) (e.g., sertraline, fluoxetine, paroxetine, citalopram, escitalopram) – premature ejaculation, paraphilias, hypersexuality, sexual deviance^[24][25][26]
• Selegiline (L-deprenyl; Eldepryl, Zelapar, Emsam) – monoamine oxidase B (MAO-B) inhibitor, other actions – low sexual desire ^[40]
• Tramadol (Tramal) – μ-opioid receptor agonist, serotonin–norepinephrine reuptake inhibitor (SNRI), other actions – premature ejaculation ^{[41][42][43][44][45][46][47]}
• Trazodone (Desyrel, Oleptro) – serotonin antagonist and reuptake inhibitor (SARI), various actions – erectile dysfunction, low sexual desire ^[48][49][50]