BCRP/ABCG2 Inducers

DrugDrug NameDrug Indication
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).
DB04540CholesterolNot Available
DB00285VenlafaxineVenlafaxine is indicated in the management of major depressive disorder (MDD), generalized anxiety disorder (GAD), social anxiety disorder (social phobia), and panic disorder with or without agoraphobia. Venlafaxine is also used off-label for prophylaxis of migraine headaches [A177229], for reduction of vasomotor symptoms associated with menopause [A177238], and for management of neuropathic pain (although there is only minimal evidence of efficacy for this condition) [A177232]. It is also considered a second-line option for management of obsessive-compulsive disorder (OCD) [A177226, A177235].
DB11901ApalutamideIndicated for the treatment of patients with non-metastatic, castration-resistant prostate cancer (NM-CRPC) [FDA Label].
DB05928DovitinibInvestigated for use/treatment in multiple myeloma and solid tumors.
DB00396Progesterone**Gelatinized capsules** The gelatinized capsules are indicated for use in the prevention of endometrial hyperplasia in non-hysterectomized postmenopausal women who are receiving conjugated estrogens tablets. They are also indicated for use in secondary amenorrhea [FDA label]. **Vaginal gel** Progesterone gel (8%) is indicated as progesterone supplementation or replacement as part of an Assisted Reproductive Technology (“ART”) treatment for infertile women with progesterone deficiency. The lower concentration progesterone gel (4%) is used in the treatment of secondary amenorrhea, with the use of the 8% concentration if there is no therapeutic response to the 4% gel [F3898]. **Vaginal insert** This form is indicated to support embryo implantation and early pregnancy by supplementation of corpus luteal function as part of an Assisted Reproductive Technology (ART) treatment program for infertile women [F3901]. **Injection (intramuscular)** This drug is indicated in amenorrhea and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology, such as submucous fibroids or uterine cancer [F3907]. **Tablets, contraceptive** The tablet form of progesterone in contraceptive formulations is indicated for the prevention of pregnancy [F3904].
DrugDrug NameTargetType
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
DB04540CholesterolNuclear receptor ROR-alphatarget
DB04540CholesterolMultidrug resistance protein 1transporter
DB04540CholesterolATP-binding cassette sub-family G member 2transporter
DB04540CholesterolNuclear receptor subfamily 1 group I member 3target
DB04540CholesterolVitamin D3 receptortarget
DB04540CholesterolC-type lectin domain family 4 member Etarget
DB00285VenlafaxineSodium-dependent serotonin transportertarget
DB00285VenlafaxineSodium-dependent noradrenaline transportertarget
DB00285VenlafaxineCytochrome P450 2D6enzyme
DB00285VenlafaxineCytochrome P450 3A4enzyme
DB00285VenlafaxineSodium-dependent dopamine transportertarget
DB00285VenlafaxineMultidrug resistance protein 1transporter
DB00285VenlafaxineATP-binding cassette sub-family G member 2transporter
DB11901ApalutamideAndrogen receptortarget
DB11901ApalutamideCytochrome P450 3A4enzyme
DB11901ApalutamideCytochrome P450 2C8enzyme
DB11901ApalutamideCytochrome P450 2C19enzyme
DB11901ApalutamideCytochrome P450 2C9enzyme
DB11901ApalutamideMultidrug resistance protein 1transporter
DB11901ApalutamideATP-binding cassette sub-family G member 2transporter
DB11901ApalutamideSolute carrier organic anion transporter family member 1B1transporter
DB11901ApalutamideSolute carrier family 22 member 2transporter
DB11901ApalutamideSolute carrier family 22 member 8transporter
DB11901ApalutamideMultidrug and toxin extrusion protein 2transporter
DB11901ApalutamideGABA-A receptor (anion channel)target
DB05928DovitinibCytochrome P450 1A1enzyme
DB05928DovitinibCytochrome P450 1A2enzyme
DB05928DovitinibCanalicular multispecific organic anion transporter 2transporter
DB05928DovitinibATP-binding cassette sub-family G member 2transporter
DB05928DovitinibUDP-glucuronosyltransferase 1-3enzyme
DB05928DovitinibUDP-glucuronosyltransferase 2B7enzyme
DB05928DovitinibNuclear receptor subfamily 1 group I member 2target
DB05928DovitinibSolute carrier organic anion transporter family member 1B1transporter
DB05928DovitinibSolute carrier organic anion transporter family member 2B1transporter
DB05928DovitinibCytochrome P450 2C19enzyme
DB05928DovitinibCytochrome P450 3A4enzyme
DB05928DovitinibSolute carrier organic anion transporter family member 1B3transporter
DB05928DovitinibMultidrug resistance protein 1transporter
DB00396ProgesteroneProgesterone receptortarget
DB00396ProgesteroneEstrogen receptor alphatarget
DB00396ProgesteroneSteroid 17-alpha-hydroxylase/17,20 lyasetarget
DB00396ProgesteroneCytochrome P450 2C19enzyme
DB00396ProgesteroneCytochrome P450 2C9enzyme
DB00396ProgesteroneCytochrome P450 3A4enzyme
DB00396ProgesteroneCytochrome P450 3A5enzyme
DB00396ProgesteroneCytochrome P450 3A7enzyme
DB00396ProgesteroneMultidrug resistance protein 1transporter
DB00396ProgesteroneSolute carrier family 22 member 2transporter
DB00396ProgesteroneSolute carrier family 22 member 1transporter
DB00396ProgesteroneSolute carrier family 22 member 3transporter
DB00396ProgesteroneBile salt export pumptransporter
DB00396ProgesteroneMultidrug resistance-associated protein 1transporter
DB00396ProgesteroneSodium/bile acid cotransportertransporter
DB00396ProgesteroneSteroid 17-alpha-hydroxylase/17,20 lyaseenzyme
DB00396ProgesteroneCytochrome P450 1A1enzyme
DB00396ProgesteroneCytochrome P450 1B1enzyme
DB00396ProgesteroneCytochrome P450 2A6enzyme
DB00396ProgesteroneCytochrome P450 2D6enzyme
DB00396ProgesteroneMineralocorticoid receptortarget
DB00396ProgesteroneKappa-type opioid receptortarget
DB00396ProgesteroneAlpha-1-acid glycoprotein 1target
DB00396ProgesteroneGlucocorticoid receptortarget
DB00396ProgesteroneAndrogen receptortarget
DB00396ProgesteroneSex hormone-binding globulintarget
DB00396ProgesteroneSolute carrier organic anion transporter family member 1B1transporter
DB00396ProgesteroneATP-binding cassette sub-family G member 2transporter
DB00396ProgesteroneEstrogen receptor betatarget
DB00396ProgesteroneSolute carrier organic anion transporter family member 1B3transporter