Progestogens and Estrogens, Sequential Preparations

DrugDrug NameDrug Indication
DB00304DesogestrelOral desogestrel is used in combination with [ethinylestradiol] as a contraceptive agent for the prevention of pregnancy.[FDA label] Desogestrel is part of the combined oral contraceptives that contain a mix of estrogen and progestin which inhibit ovulation.[L5698]
DB00351Megestrol acetateFor the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used for the palliative management of recurrent, inoperable, or metastatic breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
DB00378DydrogesteroneUsed to treat irregular duration of cycles and irregular occurrence and duration of periods caused by progesterone deficiency. Also used to prevent natural abortion in patients who have a history of habitual abortions.
DB06730GestodeneNot Available
DB12474LynestrenolNot Available
DB13129TrimegestoneNot Available
DB00367LevonorgestrelFor the treatment of menopausal and postmenopausal disorders and alone or in combination with other hormones as an oral contraceptive.
DB00717NorethisteroneFor the treatment of secondary amenorrhea, endometriosis, and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer.
DB00783EstradiolEstradiol is indicated for the treatment of moderate to severe vasomotor symptoms and vulvar and vaginal atrophy due to menopause, for the treatment of hypoestrogenism due to hypogonadism, castration, or primary ovarian failure, and for the prevention of post-menopausal osteoarthritis. It is also used for the treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease, and for the treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only).
DB00977EthinylestradiolFor treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.
DB09123DienogestIndicated for use as the treatment of endometriosis alone and as a contraceptive in combination with ethinylestradiol.
DB09124MedrogestoneMedrogestone is indicated as adjunct to treat endometial shedding in menopausal women, to treat secondary amenorrhea, to induce menses and to treat dysfunctional uterine bleeding in adult and adolescent women.[T76]
DB09389NorgestrelNorgestrel in combination with ethinyl estradiol is indicated for the prevention of pregnancy in women who elect to use this product as a method of contraception.
DB11636NomegestrolNot Available
DB13528ChlormadinoneNot Available
DB00957NorgestimateFor the prevention of pregnancy
DrugDrug NameTargetType
DB00304DesogestrelProgesterone receptortarget
DB00304DesogestrelEstrogen receptor alphatarget
DB00304DesogestrelCytochrome P450 3A4enzyme
DB00304DesogestrelSerum albumincarrier
DB00304DesogestrelSex hormone-binding globulincarrier
DB00304DesogestrelCytochrome P450 2C9enzyme
DB00304DesogestrelUDP-glucuronosyltransferase 1-1enzyme
DB00351Megestrol acetateProgesterone receptortarget
DB00351Megestrol acetateGlucocorticoid receptortarget
DB00351Megestrol acetateMultidrug resistance protein 1transporter
DB00351Megestrol acetateCytochrome P450 3A4enzyme
DB00378DydrogesteroneProgesterone receptortarget
DB00378DydrogesteroneCytochrome P450 3A4enzyme
DB06730GestodeneCytochrome P450 3A5enzyme
DB06730GestodeneCytochrome P450 3A7enzyme
DB06730GestodeneProgesterone receptortarget
DB06730GestodeneCytochrome P450 3A4enzyme
DB12474LynestrenolCytochrome P450 3A4enzyme
DB12474LynestrenolCytochrome P450 2C9enzyme
DB12474LynestrenolCytochrome P450 2C19enzyme
DB00367LevonorgestrelProgesterone receptortarget
DB00367LevonorgestrelEstrogen receptor alphatarget
DB00367Levonorgestrel3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB00367LevonorgestrelCytochrome P450 3A4enzyme
DB00367LevonorgestrelCytochrome P450 19A1enzyme
DB00367LevonorgestrelAndrogen receptortarget
DB00367LevonorgestrelSex hormone-binding globulintarget
DB00717NorethisteroneProgesterone receptortarget
DB00717NorethisteroneCytochrome P450 3A4enzyme
DB00717NorethisteroneMultidrug resistance protein 1transporter
DB00717NorethisteroneCytochrome P450 2C19enzyme
DB00717NorethisteroneCytochrome P450 3A5enzyme
DB00717NorethisteroneCytochrome P450 3A7enzyme
DB00717NorethisteroneSerum albumincarrier
DB00717NorethisteroneSex hormone-binding globulincarrier
DB00783EstradiolEstrogen receptor alphatarget
DB00783EstradiolNuclear receptor subfamily 1 group I member 2target
DB00783EstradiolSex hormone-binding globulincarrier
DB00783EstradiolEstrogen receptor betatarget
DB00783EstradiolCytochrome P450 1A2enzyme
DB00783EstradiolUDP-glucuronosyltransferase 1-1enzyme
DB00783EstradiolSerum albumincarrier
DB00783EstradiolFatty acid-binding protein, intestinalcarrier
DB00783EstradiolCytochrome P450 3A4enzyme
DB00783EstradiolCytochrome P450 3A5enzyme
DB00783EstradiolCytochrome P450 3A7enzyme
DB00783EstradiolSolute carrier family 22 member 2transporter
DB00783EstradiolSolute carrier family 22 member 1transporter
DB00783EstradiolSolute carrier family 22 member 3transporter
DB00783EstradiolSolute carrier organic anion transporter family member 2B1transporter
DB00783EstradiolSolute carrier organic anion transporter family member 1A2transporter
DB00783EstradiolMultidrug resistance-associated protein 7transporter
DB00783EstradiolSolute carrier family 22 member 11transporter
DB00783EstradiolATP-binding cassette sub-family G member 2transporter
DB00783EstradiolSolute carrier organic anion transporter family member 1B1transporter
DB00783EstradiolMultidrug resistance protein 1transporter
DB00783EstradiolCytochrome P450 1A1enzyme
DB00783EstradiolCytochrome P450 1B1enzyme
DB00783EstradiolCytochrome P450 2C19enzyme
DB00783EstradiolCytochrome P450 2C8enzyme
DB00783EstradiolCytochrome P450 2C9enzyme
DB00783EstradiolSolute carrier family 22 member 8transporter
DB00783EstradiolSolute carrier organic anion transporter family member 1B3transporter
DB00783EstradiolSolute carrier organic anion transporter family member 1C1transporter
DB00783EstradiolSolute carrier organic anion transporter family member 4A1transporter
DB00783EstradiolNeuronal acetylcholine receptor subunit alpha-4target
DB00783EstradiolNuclear receptor coactivator 2target
DB00783EstradiolG-protein coupled estrogen receptor 1target
DB00783EstradiolATP synthase subunit atarget
DB00783EstradiolBeclin-1target
DB00783EstradiolEstradiol 17-beta-dehydrogenase 2target
DB00783EstradiolEstrogen-related receptor gammatarget
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
DB00977EthinylestradiolMultidrug resistance protein 1transporter
DB00977EthinylestradiolSex hormone-binding globulintarget
DB00977EthinylestradiolUDP-glucuronosyltransferase 1-1enzyme
DB09123DienogestCytochrome P450 3A4enzyme
DB09123DienogestProgesterone receptortarget
DB09123DienogestAndrogen receptortarget
DB09124MedrogestoneSerum albumincarrier
DB09124MedrogestoneProgesterone receptortarget
DB09124MedrogestoneSex hormone-binding globulincarrier
DB09124MedrogestoneCorticosteroid-binding globulincarrier
DB09124MedrogestoneCytochrome P450 3A4enzyme
DB09389NorgestrelProgesterone receptortarget
DB09389Norgestrel3-oxo-5-alpha-steroid 4-dehydrogenase 1target
DB09389NorgestrelAndrogen receptortarget
DB09389NorgestrelCytochrome P450 3A4enzyme
DB09389NorgestrelCytochrome P450 19A1enzyme
DB11636NomegestrolCytochrome P450 3A4enzyme
DB13528ChlormadinoneCytochrome P450 3A4enzyme
DB00957NorgestimateProgesterone receptortarget
DB00957NorgestimateEstrogen receptor alphatarget
DB00957NorgestimateCanalicular multispecific organic anion transporter 1transporter
DB00957NorgestimateCytochrome P450 3A4enzyme
DB00957NorgestimateAndrogen receptortarget