Global InformationAntiandrogen information
| Antiandrogen | |
|---|---|
| Drug class | |
 Bicalutamide, a nonsteroidal antiandrogen and the most widely used androgen receptor antagonist in the treatment of prostate cancer. | |
| Class identifiers | |
| Synonyms | Androgen antagonists; Androgen blockers; Testosterone blockers |
| Use | • Men and boys: Prostate cancer; Benign prostatic hyperplasia; Scalp hair loss; Paraphilias; Hypersexuality; Sex offenders; Precocious puberty; Priapism • Women and girls: Acne; Seborrhea; Hidradenitis suppurativa; Hirsutism; Scalp hair loss; Hyperandrogenism; Transgender hormone therapy |
| ATC code | L02BB |
| Biological target | Androgen receptor; Progesterone receptor; Estrogen receptor; GnRH receptor; 5α-Reductase; CYP17A1 (17α-hydroxylase/ |
| Chemical class | Steroidal; Nonsteroidal; Peptide |
| External links | |
| MeSH | D000726 |
| Legal status | |
| In Wikidata | |
Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. They act by blocking the androgen receptor (AR) and/or inhibiting or suppressing androgen production.[1][2] They can be thought of as the functional opposites of AR agonists, for instance androgens and anabolic steroids (AAS) like testosterone, DHT, and nandrolone and selective androgen receptor modulators (SARMs) like enobosarm. Antiandrogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiprogestogens.[3]
Antiandrogens are used to treat an assortment of androgen-dependent conditions.[4] In men, antiandrogens are used in the treatment of prostate cancer, enlarged prostate, scalp hair loss, overly high sex drive, unusual and problematic sexual urges, and early puberty.[4][5] In women, antiandrogens are used to treat acne, seborrhea, excessive hair growth, scalp hair loss, and high androgen levels, such as those that occur in polycystic ovary syndrome (PCOS).[4] Antiandrogens are also used as a component of feminizing hormone therapy for transgender women and as puberty blockers in transgender girls.[4]
Side effects of antiandrogens depend on the type of antiandrogen and the specific antiandrogen in question. In any case, common side effects of antiandrogens in men include breast tenderness, breast enlargement, feminization, hot flashes, sexual dysfunction, infertility, and osteoporosis. In women, antiandrogens are much better tolerated, and antiandrogens that work only by directly blocking androgens are associated with minimal side effects. However, because estrogens are made from androgens in the body, antiandrogens that suppress androgen production can cause low estrogen levels and associated symptoms like hot flashes, menstrual irregularities, and osteoporosis in premenopausal women.
There are a few different major types of antiandrogens.[6] These include AR antagonists, androgen synthesis inhibitors, and antigonadotropins.[6] AR antagonists work by directly blocking the effects of androgens, while androgen synthesis inhibitors and antigonadotropins work by lowering androgen levels.[6] AR antagonists can be further divided into steroidal antiandrogens and nonsteroidal antiandrogens; androgen synthesis inhibitors can be further divided mostly into CYP17A1 inhibitors and 5α-reductase inhibitors; and antigonadotropins can be further divided into gonadotropin-releasing hormone modulators (GnRH modulators), progestogens, and estrogens.[6][7][8]
- ^ Mowszowicz I (1989). "Antiandrogens. Mechanisms and paradoxical effects". Ann. Endocrinol. 50 (3). Paris: 50(3):189–99. PMID 2530930.
- ^ Brueggemeier RW (2006). "Sex Hormones (Male): Analogs and Antagonists". Encyclopedia of Molecular Cell Biology and Molecular Medicine. doi:10.1002/3527600906.mcb.200500066. ISBN 3527600906.
- ^ Nath JL (2006). Using Medical Terminology: A Practical Approach. Lippincott Williams & Wilkins. pp. 977–. ISBN 978-0-7817-4868-1.
- ^ a b c d Student S, Hejmo T, Poterała-Hejmo A, Leśniak A, Bułdak R (January 2020). "Anti-androgen hormonal therapy for cancer and other diseases". Eur. J. Pharmacol. 866: 172783. doi:10.1016/j.ejphar.2019.172783. PMID 31712062.
- ^ Gillatt D (2006). "Antiandrogen treatments in locally advanced prostate cancer: are they all the same?". J Cancer Res Clin Oncol. 1: S17-26. doi:10.1007/s00432-006-0133-5. PMID 16845534. S2CID 23888640.
- ^ a b c d Lieberman R (2001). "Androgen deprivation therapy for prostate cancer chemoprevention: current status and future directions for agent development". Urology. 58 (2 Suppl 1): 83–90. doi:10.1016/s0090-4295(01)01247-x. PMID 11502457.
There are several classes of antiandrogens including (1) antigonadotropins (eg, LHRH agonists/antagonists, synthetic estrogens [diethylstilbestrol]); (2) nonsteroidal androgen-receptor antagonists (eg, flutamide, bicalutamide, nilutamide); (3) steroidal agents with mixed actions (eg, cyproterone acetate); (4) adrenal androgen inhibitors (eg, ketoconazole, hydrocortisone); (5) steroidal agents that inhibit androgen biosynthesis (eg, 5α-reductase inhibitors (type II) and dual-acting 5α-reductase inhibitors); [...]
- ^ Schröder FH, Radlmaier A (2009). "Steroidal Antiandrogens". In Jordan VC, Furr BA (eds.). Hormone Therapy in Breast and Prostate Cancer. Humana Press. pp. 325–346. doi:10.1007/978-1-59259-152-7_15. ISBN 978-1-60761-471-5.
- ^ Kolvenbag GJ, Furr BJ (2009). "Nonsteroidal Antiandrogens". In Jordan VC, Furr BJ (eds.). Hormone Therapy in Breast and Prostate Cancer. Humana Press. pp. 347–368. doi:10.1007/978-1-59259-152-7_16. ISBN 978-1-60761-471-5.