Heavy Menstrual Bleeding

Also known as: Bleeding menstrual heavy / Menorrhagia / Heavy periods NOS / Hypermenorrhea / Menstrual flow excessive / Hypermenorrhoea / Heavy periods / Excessive menstruation / Menses regular with excessive bleeding / Prolonged heavy periods / Menstruation increased

DrugDrug NameDrug Description
DB13956Estradiol valerateEstradiol Valerate (also known as E2V) is a pro-drug ester of [DB00783], a naturally occurring hormone that circulates endogenously within the human body. Estradiol is the most potent form of all mammalian estrogenic steroids and acts as the major female sex hormone. As a pro-drug of estradiol, estradiol acetate therefore has the same downstream effects within the body through binding to the Estrogen Receptor (ER) including ERα and ERβ subtypes, which are located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. [DB00783] is commonly produced with an ester side-chain as endogenous estradiol has very low oral bioavailability on its own (2-10%). First-pass metabolism by the gut and the liver quickly degrades the estradiol molecule before it gets a chance to enter systemic circulation and exert its estrogenic effects [A12102]. Esterification of estradiol aims to improves absorption and bioavailability after oral administration (such as with Estradiol valerate) or to sustain release from depot intramuscular injections (such as with Estradiol Cypionate) through improved lipophilicity. Following absorption, the esters are cleaved, resulting in the release of endogenous estradiol, or 17β-estradiol. Ester pro-drugs of estradiol are therefore considered to be bioidentical forms of estrogen [T84]. Estradiol valerate is commercially available as an intramuscular injection as the product Delestrogen and is indicated for the treatment of moderate to severe vasomotor symptoms and vulvovaginal atrophy due to menopause, for the treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure, and for the treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only). Estradiol valerate is also available in combination with [DB09123] as the commercially available product Natazia used for the prevention of pregnancy and for the treatment of heavy menstrual bleeding. The primary source of estrogen in normally cycling adult women is the ovarian follicle, which secretes 70 to 500 mcg of estradiol daily, depending on the phase of the menstrual cycle. However, after menopause, most endogenous estrogen is produced by conversion of androstenedione, secreted by the adrenal cortex, to estrone by peripheral tissues. Thus, estrone and the sulfate conjugated form, estrone sulfate, are the most abundant circulating estrogens in postmenopausal women [FDA Label]. Although circulating estrogens exist in a dynamic equilibrium of metabolic interconversions, estradiol is the principal intracellular human estrogen and is substantially more potent than its metabolites, estrone and estriol at the receptor level. Because of the difference in potency between estradiol and estrone, menopause (and a change in primary hormone from estradiol to estrone) is associated with a number of symptoms associated with this reduction in potency and in estrogenic effects. These include hot flashes, vaginal dryness, mood changes, irregular menses, chills, and sleeping problems. Administration of synthetic and bioidentical forms of estrogen, such as estradiol valerate, has shown to improve these menopausal symptoms.
DrugDrug NameTargetType
DB13956Estradiol valerateEstrogen receptor alphatarget
DB13956Estradiol valerateNuclear receptor subfamily 1 group I member 2target
DB13956Estradiol valerateSex hormone-binding globulincarrier
DB13956Estradiol valerateEstrogen receptor betatarget
DB13956Estradiol valerateCytochrome P450 1A2enzyme
DB13956Estradiol valerateUDP-glucuronosyltransferase 1-1enzyme
DB13956Estradiol valerateSerum albumincarrier
DB13956Estradiol valerateFatty acid-binding protein, intestinalcarrier
DB13956Estradiol valerateCytochrome P450 3A4enzyme
DB13956Estradiol valerateCytochrome P450 3A5enzyme
DB13956Estradiol valerateCytochrome P450 3A7enzyme
DB13956Estradiol valerateSolute carrier family 22 member 2transporter
DB13956Estradiol valerateSolute carrier family 22 member 1transporter
DB13956Estradiol valerateSolute carrier family 22 member 3transporter
DB13956Estradiol valerateSolute carrier organic anion transporter family member 2B1transporter
DB13956Estradiol valerateSolute carrier organic anion transporter family member 1A2transporter
DB13956Estradiol valerateMultidrug resistance-associated protein 7transporter
DB13956Estradiol valerateSolute carrier family 22 member 11transporter
DB13956Estradiol valerateATP-binding cassette sub-family G member 2transporter
DB13956Estradiol valerateSolute carrier organic anion transporter family member 1B1transporter
DB13956Estradiol valerateMultidrug resistance protein 1transporter
DB13956Estradiol valerateCytochrome P450 1A1enzyme
DB13956Estradiol valerateCytochrome P450 1B1enzyme
DB13956Estradiol valerateCytochrome P450 2C19enzyme
DB13956Estradiol valerateCytochrome P450 2C8enzyme
DB13956Estradiol valerateCytochrome P450 2C9enzyme
DB13956Estradiol valerateSolute carrier family 22 member 8transporter
DB13956Estradiol valerateSolute carrier organic anion transporter family member 1B3transporter
DB13956Estradiol valerateSolute carrier organic anion transporter family member 1C1transporter
DB13956Estradiol valerateSolute carrier organic anion transporter family member 4A1transporter
DB13956Estradiol valerateNeuronal acetylcholine receptor subunit alpha-4target
DB13956Estradiol valerateNuclear receptor coactivator 2target
DB13956Estradiol valerateG-protein coupled estrogen receptor 1target
DB13956Estradiol valerateATP synthase subunit atarget
DB13956Estradiol valerateBeclin-1target
DB13956Estradiol valerateEstradiol 17-beta-dehydrogenase 2target
DB13956Estradiol valerateEstrogen-related receptor gammatarget
DrugDrug NamePhaseStatusCount
DB10580Tea leaf1Not Yet Recruiting1
DB08837Tetraethylammonium1Not Yet Recruiting1
DB00302Tranexamic acid1Not Yet Recruiting1
DB08867Ulipristal1Not Yet Recruiting1
DB00013Urokinase1Not Yet Recruiting1
DB11979Elagolix3Active Not Recruiting2
DB00603Medroxyprogesterone acetate3Recruiting1
DB00784Mefenamic acid3Recruiting1
DB11853Relugolix3Active Not Recruiting2
DB11853Relugolix3Enrolling by Invitation1
DB00302Tranexamic acid3Completed3
DB00717Norethisterone4Unknown Status1
DB00302Tranexamic acid4Completed1
DB00302Tranexamic acid4Recruiting1
DB00802AlfentanilNot AvailableRecruiting1
DB00479AmikacinNot AvailableRecruiting1
DB00513Aminocaproic AcidNot AvailableRecruiting1
DB00559BosentanNot AvailableRecruiting1
DB01413CefepimeNot AvailableRecruiting1
DB00369CidofovirNot AvailableRecruiting1
DB00537CiprofloxacinNot AvailableRecruiting1
DB00363ClozapineNot AvailableRecruiting1
DB00828FosfomycinNot AvailableRecruiting1
DB00502HaloperidolNot AvailableRecruiting1
DB00598LabetalolNot AvailableRecruiting1
DB08815LurasidoneNot AvailableRecruiting1
DB00959MethylprednisoloneNot AvailableRecruiting1
DB01618MolindoneNot AvailableRecruiting1
DB00607NafcillinNot AvailableRecruiting1
DB01115NifedipineNot AvailableRecruiting1
DB00497OxycodoneNot AvailableRecruiting1
DB00312PentobarbitalNot AvailableRecruiting1
DB00728RocuroniumNot AvailableRecruiting1
DB00658SevelamerNot AvailableRecruiting1
DB00421SpironolactoneNot AvailableRecruiting1
DB00684TobramycinNot AvailableRecruiting1
DB00302Tranexamic acidNot AvailableRecruiting1
DB00512VancomycinNot AvailableRecruiting1
DB01339VecuroniumNot AvailableRecruiting1
DB00682WarfarinNot AvailableRecruiting1
DB00246ZiprasidoneNot AvailableRecruiting1
DB00425ZolpidemNot AvailableRecruiting1