Polycystic Ovarian Syndrome

Also known as: PCOS / Sclerocystic ovary syndrome / Stein-Leventhal syndrome / Multicystic ovaries / Polycystic ovaries / Polycystic ovary / Polycystic Ovary Syndrome

DrugDrug NameDrug Description
DB01395DrospirenoneDrospirenone is a synthetic progestin commonly found in the popular oral contraceptive, Yaz in combination with [Ethinyl estradiol].[L7973] Aside from its contraceptive effects, drospirenone is used with estrogens to control acne and premenstrual dysphoric disorder (PMDD). Drospirenone has been the subject of widespread safety concern due to the possibility of an increased risk of venous thromboembolism associated with its use.[A182543,A182552] In 2012, however, a safety statement by the FDA concluded that the increase in the risk of thromboembolism resulting from the use of drospirenone remains unclear, as studies regarding this risk are conflicting. Some studies have demonstrated a significantly increased risk and some demonstrating no risk of thromboembolic events. In its statement, the FDA has mentioned that increased risk of venous thromboembolism with oral contraceptives such as drospirenone exists but remains lower than the risk of this condition during pregnancy and during the postpartum period, and this should be considered when assessing potential risks of hormonal contraceptive use.[L7979]
DB00977EthinylestradiolA semisynthetic alkylated estradiol with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally and is often used as the estrogenic component in oral contraceptives. Ethinyl estradiol is marketed mostly as a combination oral contraceptive under several brand names such as Alesse, Tri-Cyclen, Triphasil, and Yasmin. The FDA label includes a black box warning that states that combination oral contraceptives should not be used in women over 35 years old who smoke due to the increased risk of serious cardiovascular side effects.
DB00823Ethynodiol diacetateA synthetic progestational hormone used alone or in combination with estrogens as an oral contraceptive. Although etynodiol or ethynodiol are sometimes used as a synonym for ethynodiol diacetate, what is usually being referred to is actually ethynodiol diacetate and not ethynodiol (which is a separate drug that has never been marketed, see [DB13866]).
DB01216FinasterideFinasteride is a synthetic 4-azasteroid compound[Label] and specific inhibitor of steroid Type II 5α-reductase, which is an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (DHT). It works in a similar fashion as [dutasteride], which is another 5-alpha-reductase inhibitor, by exerting antiandrogenic effects. Finasteride is an orally active drug that was first approved by the FDA in 1992 for the treatment of benign prostatic hyperplasia to improve symptoms and reduce the risk for acute urinary retention or the need for surgical procedures.[Label,L6244] In 1998, it was approved by the FDA to treat male pattern hair loss.[L6244] Finasteride is commonly marketed under the brand names Propecia and Proscar to be used aloneo or in combination with [doxazosin], an alpha-blocker. Both benign prostatic hyperplasia and androgenic alopecia are androgen-dependent disorders that are characterized by _in situ_ high levels of DHT.[A178159] In the treatment of benign prostate hyperplasia, alpha-blockers such as [tamsulosin] and [terazosin] are also used. Compared to alpha-blockers that focus on providing the rapid relief of symptoms, 5α-reductase inhibitors aim to target the underlying disease by blocking the effects of the primary androgen involved in benign prostate hyperplasia and androgenic alopecia, thus reducing the risk for secondary complications while providing symptom control.[A2132]
DB01006LetrozoleLetrozole (INN, trade name Femara®) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant treatment of hormonally-responsive breast cancer Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Letrozole blocks the production of estrogens in this way by competitive, reversible binding to the heme of its cytochrome P450 unit. It is important to note that letrozole does not decrease the production of mineralocorticoids or corticosteroids. In contrast, the antiestrogenic action of tamoxifen, the major medical therapy prior to the arrival of aromatase inhibitors, is due to its interfering with the estrogen receptor, rather than inhibiting estrogen production. Side effects include signs and symptoms of hypoestrogenism. There is concern that long term use may lead to osteoporosis, which is why prescriptions of Letrozole are often accompanied by prescriptions of osteoporosis-fighting medication such as Fosamax. Letrozole has shown to reduce estrogen levels by 98 percent while raising testosterone levels. The anti-estrogen action of letrozole is preferred by athletes and bodybuilders for use during a steroid cycle to reduce bloating due to excess water retention and prevent the formation of gynecomastia related breast tissue that is a side effect of some anabolic steroids. Usage above 2.5 mg/day is known to potentially temporarily kill sex drive. Above 5mg/day for extended periods may cause kidney problems. Letrozole has also been shown to delay the fusing of the growth plates in adolescents. This may boost the effectiveness of growth hormone, and thus Letrozole is used to treat adolescents and children with short stature.
DB01357MestranolThe 3-methyl ether of ethinyl estradiol. It must be demethylated to be biologically active. It is used as the estrogen component of many combination ORAL contraceptives.
DB06713NorelgestrominNorelgestromin is a drug used in contraception. Norelgestromin is the active progestin responsible for the progestational activity that occurs in women after application of ORTHO EVRA patch.
DB00957NorgestimateNorgestimate is a form of progesterone, which is a female hormone important for the regulation of ovulation and menstruation. Norgestimate is used with estradiol to treat the symptoms of menopause.
DB09389NorgestrelNorgestrel is synthetic steroidal progestin that is used in combination with ethinyl estradiol for oral contraception. Norgestrel is composed of a racemic mixture of two stereoisomers, dextronorgestrel and levonorgestrel. However, only the levorotary enantiomer ([levonorgestrel]) is biologically active.
DrugDrug NameTargetType
DB01395DrospirenoneProgesterone receptortarget
DB01395DrospirenoneMineralocorticoid receptortarget
DB01395DrospirenoneAndrogen receptortarget
DB01395DrospirenoneProstaglandin G/H synthase 2enzyme
DB01395DrospirenoneSerum paraoxonase/arylesterase 1enzyme
DB01395DrospirenoneGlucocorticoid receptortarget
DB01395DrospirenoneCytochrome P450 3A4enzyme
DB00977EthinylestradiolEstrogen receptor alphatarget
DB00977EthinylestradiolNuclear receptor subfamily 1 group I member 2target
DB00977EthinylestradiolCytochrome P450 3A4enzyme
DB00977EthinylestradiolCytochrome P450 2C8enzyme
DB00977EthinylestradiolBile salt export pumptransporter
DB00977EthinylestradiolSodium/bile acid cotransportertransporter
DB00977EthinylestradiolCanalicular multispecific organic anion transporter 1transporter
DB00977EthinylestradiolP-glycoprotein 1transporter
DB00977EthinylestradiolSex hormone-binding globulintarget
DB00977EthinylestradiolUDP-glucuronosyltransferase 1-1enzyme
DB00977EthinylestradiolCytochrome P450 2C19enzyme
DB00823Ethynodiol diacetateEstrogen receptor alphatarget
DB00823Ethynodiol diacetateProgesterone receptortarget
DB00823Ethynodiol diacetateCytochrome P450 3A4enzyme
DB01216Finasteride3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB01216FinasterideCytochrome P450 3A4enzyme
DB01216Finasteride3-oxo-5-alpha-steroid 4-dehydrogenase 2target
DB01216Finasteride3-oxo-5-beta-steroid 4-dehydrogenasetarget
DB01216FinasterideCytochrome P450 3A5enzyme
DB01216FinasterideCytochrome P450 3A7enzyme
DB01216FinasterideSolute carrier family 12 member 5transporter
DB01006LetrozoleCytochrome P450 19A1target
DB01006LetrozoleCytochrome P450 3A4enzyme
DB01006LetrozoleCytochrome P450 2A6enzyme
DB01006LetrozoleCytochrome P450 19A1enzyme
DB01357MestranolEstrogen receptor alphatarget
DB01357MestranolCytochrome P450 2C9enzyme
DB01357MestranolCytochrome P450 3A4enzyme
DB01357MestranolCytochrome P450 2C8enzyme
DB06713NorelgestrominProgesterone receptortarget
DB06713NorelgestrominSerum albumintarget
DB06713NorelgestrominAndrogen receptortarget
DB06713NorelgestrominCytochrome P450 3A4enzyme
DB00957NorgestimateProgesterone receptortarget
DB00957NorgestimateEstrogen receptor alphatarget
DB00957NorgestimateCanalicular multispecific organic anion transporter 1transporter
DB00957NorgestimateCytochrome P450 3A4enzyme
DB00957NorgestimateAndrogen receptortarget
DB09389NorgestrelProgesterone receptortarget
DB09389Norgestrel3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB09389NorgestrelAndrogen receptortarget
DB09389NorgestrelCytochrome P450 3A4enzyme
DB09389NorgestrelCytochrome P450 19A1enzyme
DrugDrug NamePhaseStatusCount
DB00331Metformin0Not Yet Recruiting1
DB00331Metformin0Unknown Status1
DB00882Clomifene1Unknown Status1
DB00882Clomifene2Not Yet Recruiting1
DB04839Cyproterone acetate2Active Not Recruiting1
DB04839Cyproterone acetate2Recruiting1
DB00977Ethinylestradiol2Active Not Recruiting1
DB11094Vitamin D2Completed1
DB15350D-chiro-Inositol2 / 3Completed1
DB01276Exenatide2 / 3Not Yet Recruiting1
DB01276Exenatide2 / 3Recruiting1
DB13178Inositol2 / 3Completed1
DB00331Metformin2 / 3Completed1
DB00421Spironolactone2 / 3Completed1
DB01200Bromocriptine3Unknown Status1
DB00097Choriogonadotropin alfa3Completed2
DB09126Chorionic Gonadotropin (Human)3Completed2
DB00158Folic acid3Recruiting1
DB00284Acarbose4Not Yet Recruiting1
DB09126Chorionic Gonadotropin (Human)4Recruiting1
DB09126Chorionic Gonadotropin (Human)4Withdrawn1
DB04839Cyproterone acetate4Unknown Status1
DB01395Drospirenone4Unknown Status1
DB00977Ethinylestradiol4Unknown Status1
DB01276Exenatide4Not Yet Recruiting1
DB00158Folic acid4Completed1
DB00158Folic acid4Recruiting1
DB00331Metformin4Not Yet Recruiting1
DB00331Metformin4Unknown Status2
DB01083Orlistat4Not Yet Recruiting1
DB11094Vitamin D4Recruiting2
DB00248CabergolineNot AvailableCompleted1
DB01373CalciumNot AvailableCompleted1
DB00882ClomifeneNot AvailableCompleted1
DB00882ClomifeneNot AvailableRecruiting1
DB00882ClomifeneNot AvailableTerminated1
DB06699DegarelixNot AvailableUnknown Status1
DB01119DiazoxideNot AvailableCompleted1
DB13956Estradiol valerateNot AvailableCompleted1
DB00644GonadorelinNot AvailableUnknown Status1
DB01006LetrozoleNot AvailableRecruiting1
DB01006LetrozoleNot AvailableUnknown Status1
DB00603Medroxyprogesterone acetateNot AvailableCompleted1
DB00603Medroxyprogesterone acetateNot AvailableTerminated1
DB00331MetforminNot AvailableCompleted1
DB00331MetforminNot AvailableRecruiting1
DB00393NimodipineNot AvailableCompleted1
DB00396ProgesteroneNot AvailableCompleted1
DB00481RaloxifeneNot AvailableTerminated1
DB11094Vitamin DNot AvailableCompleted1