This is a list of investigational PMS/PMDD drugs, or drugs that are currently under development for clinical use for the treatment of premenstrual syndrome (PMS) or premenstrual dysphoric disorder (PMDD) but are not yet approved.
Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. The format of list items is "Name (Synonyms) – Mechanism of Action – Indication [Reference]".
This list was last comprehensively updated in March 2026. It is likely to become outdated with time.
Under development Phase 2 Pyridoxamine (RS-8001) – vitamin B6 and antioxidant – PMS Refisolone (ORG-39479; PH-80; PH-80-M; PH80-PMD NS) – vomeropherine / "neurotransmitter receptor modulator" – PMDD Sepranolone (isoallopregnanolone; UC-1010) – GABAA receptor negative allosteric modulator and excitatory neurosteroid – PMDD
Not under development No development reported Ethinylestradiol/drospirenone (dihydrospirorenone/ethinylestradiol; drospirenone/ethinylestradiol; Petibelle; SH-470; Yasmin; ZK-30595) – combination of ethinylestradiol (estrogen) and drospirenone (progestin) – PMS and PMDD Progesterone intranasal (MetP Progesterone Nasal Gel; MPP 22; ProgestoMat) – progestogen (progesterone receptor agonist) and GABAA receptor positive allosteric modulator (via metabolites) – PMS Progesterone vaginal – progestogen (progesterone receptor agonist) and GABAA receptor positive allosteric modulator (via metabolites) – PMS Research programme: premenstrual syndrome therapeutic - Panacor Bioscience (PB301) – undefined mechanism of action – PMS
Discontinued Ethinylestradiol/levonorgestrel continuous (EE/Levo continuous; EE/LNG continuous; Levo/EE continuous; Levonorgestrel/ethinlyestradiol continuous; Librel; LNG/EE continuous; Lybrel) – combination of ethinylestradiol (estrogen) and levonorgestrel (progestin) – PMS and PMDD Progesterone transdermal (progesterone spray; Progesterone TDS®) – progestogen (progesterone receptor agonist) and GABAA receptor positive allosteric modulator (via metabolites) – PMS
Clinically used drugs Approved drugs Hormonal agents Ethinylestradiol/drospirenone low-dose (BAY86-5300; BAY86-5300-YAZ-Flex; Drospirenone/ethinylestradiol; EE20/Drospirenone; EE20/DRSP; Ethinylestradiol-Drospirenone 24+4; Flexyess; SH-T-00186D; Yasmin® 20; Yasminelle; Yaz; Yaz 24+4; Yaz Extended Cycle; YAZ Extended Regimen; Yaz Flex; Yvidually) – combination of ethinylestradiol (estrogen) and drospirenone (progestin) – PMS and PMDD Ethinylestradiol/drospirenone/levomefolic acid (BAY98-7071; Beyaz; EE20/DRSP/L-5MTHF; ethinylestradiol/drospirenone/methyltetrahydrofolate; Safyral; Yasmin Plus; Yaz Flex Plus; Yaz Plus) – combination of ethinylestradiol (estrogen), drospirenone (progestin), and levomefolic acid (vitamin B9) – PMDD Progesterone gel (COL-1620; Crinone; Crinone 4%; Crinone 8%; Crinone8%; OneCrinone; Prochieve; Prochieve4%; Prochieve8%; progesterone vaginal gel 4%; progesterone vaginal gel 8%) – progestogen (progesterone receptor agonist) and GABAA receptor positive allosteric modulator (via metabolites) – PMS Progesterone vaginal (Utrogestan) – progestogen (progesterone receptor agonist) and GABAA receptor positive allosteric modulator (via metabolites) – PMS
Antidepressants Fluoxetine (LY-110140; Prozac; Prozac Weekly; Reneuron; Sarafem) – selective serotonin reuptake inhibitor (SSRI) – PMDD Paroxetine (Aropax; BRL 29060; BRL 29060A; Deroxat; Divarius; FG 7051; Frosinor; Motivan; NNC 207051; Paxil; Paxil CR; Seroxat; SI 211103; Tagonis) – selective serotonin reuptake inhibitor (SSRI) – PMDD Sertraline (Aremis; Besitran; CP 51974; CP 51974 01; Gladem; J Zoloft; Lustral; Serad; Serlain; Tatig; Zoloft) – selective serotonin reuptake inhibitor (SSRI) – PMDD
Off-label drugs Hormonal agents 5α-Reductase inhibitors (e.g., dutasteride) (via neurosteroid synthesis inhibition) Androgens (androgen receptor agonists) (e.g., danazol) GnRH agonists (e.g., leuprorelin) and GnRH antagonists (e.g., elagolix, relugolix) (with or without add-back estrogen–progestogen therapy) Neurosteroids acting as GABAA receptor positive allosteric modulators (e.g., brexanolone (allopregnanolone), zuranolone, ganaxolone) Other contraceptive and non-contraceptive estrogen–progestogen therapies Other progesterone formulations and progestogens Selective progesterone receptor modulators (SPRMs) (e.g., ulipristal acetate) Spironolactone (Aldactone) – antimineralocorticoid (mineralocorticoid receptor antagonist), other actions
Psychiatric medications Anxiolytics (e.g., benzodiazepines (e.g., alprazolam), buspirone) Other selective serotonin reuptake inhibitors (SSRIs) (e.g., citalopram, escitalopram) Other serotonergic antidepressants (e.g., venlafaxine, duloxetine, clomipramine)
See also List of investigational drugs List of investigational sex-hormonal agents List of investigational antidepressants
References
External links AdisInsight - Springer