85 articles
Encequidar
Encequidar (HM30181) is a minimally absorbed, gut-specific P-glycoprotein inhibitor by Hanmi/Athenex that enables oral paclitaxel (Oraxol); phase III in metastatic breast cancer showed higher response and less neuropathy than IV paclitaxel; not approved.
Enobosarm
Enobosarm (ostarine, GTx-024, MK-2866, VERU-024) is an oral nonsteroidal SARM developed for cancer cachexia; it raised lean body mass in phase 2/3 trials but won no US or EU approval and is WADA-prohibited.
Feminizing hormone therapy
Feminizing hormone therapy combines 17-beta estradiol with antiandrogens such as spironolactone to develop female secondary sex characteristics and suppress testosterone in transgender women, with VTE risk shaping formulation choice.
Finasteride
Finasteride (Propecia, Proscar) is a type II 5α-reductase inhibitor lowering DHT ~70%; used at 5 mg for BPH and 1 mg for male pattern hair loss, with PSA-lowering, sexual and psychiatric side-effect debates.
Gonadotropin-releasing hormone agonist
GnRH agonists (leuprolide, goserelin, triptorelin, buserelin, nafarelin, histrelin) are D-amino-acid-substituted GnRH decapeptide analogs that flare then suppress pituitary gonadotropins, used for prostate cancer, endometriosis, fibroids, and precocious puberty.
GW501516
GW501516 (GW1516, Cardarine, Endurobol) is a potent PPARδ agonist developed by GSK and Ligand for metabolic disease, abandoned in 2007 over rodent carcinogenicity, and banned in sport by WADA since 2009.
Hexafluorenium
Hexafluorenium (Mylaxen), C36H42N2, a bis-quaternary fluorene nondepolarizing neuromuscular blocker and reversible non-competitive plasma cholinesterase inhibitor used to prolong succinylcholine; US NDA withdrawn 1994.
HGH Fragment 176–191
HGH Fragment 176-191 (hGH 176-191, Frag 176-191) is the synthetic 16-amino-acid C-terminal fragment of human growth hormone, sequence FLRIVQCRSVEGSCGF, studied for lipolytic activity; distinct from AOD-9604, with no human trials and no regulatory approval.
Hormone replacement therapy
Hormone replacement therapy (HRT, menopausal hormone therapy) replaces estrogen and progestogen to treat menopause symptoms; shaped by the 2002 WHI trial and the FDA's 2025-2026 removal of boxed warnings.
Hyoscyamine
Hyoscyamine, a tropane alkaloid from Atropa belladonna and the L-isomer of atropine, is an antimuscarinic antispasmodic used for GI spasm and IBS, with weak efficacy evidence and anticholinergic side effects.
Ibutamoren
Ibutamoren (MK-677, MK-0677, LUM-201) is an oral non-peptide ghrelin receptor agonist that raises GH and IGF-1; synthesized by Merck in 1995, discontinued in 1999, never FDA approved, and WADA-prohibited since 2013.
Imiquimod
Imiquimod (Aldara, Zyclara) is a topical imidazoquinoline immune response modifier and TLR7/8 agonist approved since 1997 for genital warts, actinic keratosis, and superficial basal cell carcinoma.
Inverse agonist
Inverse agonist: ligand lowering receptor signaling below constitutive (ligand-independent) activity, unlike neutral antagonists; defined by IUPAC, first shown at delta opioid receptor with ICI174864.
Ketamine
Ketamine, a phencyclidine-derived dissociative anesthetic and NMDA receptor antagonist (Ketalar; esketamine as Spravato), synthesized 1962, FDA-approved 1970, and repurposed since 2000 as a rapid-acting antidepressant for treatment-resistant depression and acute suicidality.
Latanoprost
Latanoprost (Xalatan) is a prostaglandin F2α analogue eye drop, first US-approved 1996, that lowers intraocular pressure in open-angle glaucoma and ocular hypertension via increased uveoscleral outflow, dosed once daily at 0.005%.
Levonorgestrel
Levonorgestrel (LNG), also known as Plan B One-Step, is a second-generation progestin used in emergency contraceptive pills (1.5 mg), LNG intrauterine systems, and former implants; it prevents pregnancy by delaying ovulation.
Mechanism of action
Mechanism of action (MOA) is the specific biochemical interaction by which a drug produces its effect, typically via receptors or enzymes; grounded in receptor theory and central to drug development.
Mechanism of action of aspirin
Mechanism of action of aspirin: irreversible acetylation of COX-1 Ser529 and COX-2 Ser516, blocking prostaglandin and thromboxane synthesis; discovered by Vane in 1971; explains analgesic, anti-inflammatory, and antiplatelet effects.
Melanotan II
Melanotan II (MT-2, MT2) is a cyclic heptapeptide analogue of alpha-MSH, a non-selective melanocortin receptor agonist studied for tanning and erectile dysfunction, never approved as a drug and sold illegally as a tanning injection.
Metandienone
Metandienone (methandrostenolone, Dianabol), 17β-hydroxy-17α-methylandrosta-1,4-dien-3-one, is an oral 17α-alkylated anabolic steroid, formerly used for hypogonadism at 2.5–5 mg/day, now discontinued medically and prohibited at all times by WADA under S1.1.
Metformin
Metformin (1,1-dimethylbiguanide), a biguanide oral drug first U.S.-approved in 1995, is the most prescribed treatment for type 2 diabetes; it weakly inhibits mitochondrial complex I, activates AMPK, inhibits hepatic gluconeogenesis, and carries a lactic acidosis boxed warning.
Methylene blue
Methylene blue, a phenothiazine dye synthesized by Caro in 1876, is the standard antidote for methemoglobinemia (1 mg/kg IV), a stain, and an investigational NO-cGMP inhibitor in vasodilatory shock with unproven mortality benefit.
Methyltestosterone
Methyltestosterone, sold under brand names including Testred and Methitest, is a synthetic oral anabolic-androgenic steroid, first synthesized in 1935, used for testosterone replacement in men and delayed puberty.
Mithridatism
Mithridatism, also called mithridatization, is self-administering gradually increased doses of a poison to gain tolerance, named after Mithridates VI of Pontus; no scientific evidence supports its success, though drug tolerance is real.
Molecular pharmacology
Molecular pharmacology: study of molecular actions and interactions of drugs, rooted in receptor theory (Langley, 1905); also the ASPET journal Molecular Pharmacology (Mol Pharmacol), founded July 1965, ISSN 0026-895X.
Nandrolone
Nandrolone (19-nortestosterone, Deca-Durabolin), an anabolic steroid synthesized in 1950, used as decanoate injections for anemia and osteoporosis, with an 11:1 anabolic-androgenic ratio, WADA prohibition, and 2 ng/ml 19-norandrosterone threshold.
Neuropharmacology
Neuropharmacology: branch of pharmacology studying drug interactions with the central and peripheral nervous systems; covers neurotransmitter mechanisms, drug classes (antidepressants, antipsychotics, antiepileptics), the blood-brain barrier, and emerging precision and AI-driven CNS therapies.
Oxandrolone
Oxandrolone (Oxandrin) is a synthetic 17-alpha-alkylated anabolic steroid, formerly FDA-approved for weight gain and corticosteroid catabolism; approval withdrawn June 2023. Best studied in burns: faster recovery, no mortality benefit, hepatotoxicity risk.
Oxymetholone
Oxymetholone (Anadrol-50) is a 17α-alkylated anabolic-androgenic steroid, a synthetic testosterone derivative once FDA-approved for anemias from deficient red cell production; now discontinued in the US, hepatotoxic, and listed as reasonably anticipated to be a human carcinogen.
Paradoxical reaction
Paradoxical reaction: an adverse drug effect opposite to the drug's expected pharmacological action, classically agitation or aggression from sedative benzodiazepines like midazolam, occurring in under 1% of patients and reversible with flumazenil.