Progonadotropin

Drug class

Progonadotropin
Drug class
Clomifene, a SERMTooltip selective estrogen receptor modulator with progonadotropic effects which is used in the treatment of infertility to induce ovulation.
Class identifiers
Synonyms	Hypergonadotropin; Gonad stimulant
Use	Hypogonadism, infertility
Chemical class	Steroidal; Nonsteroidal
Legal status
In Wikidata

A progonadotropin, or hypergonadotropin, also known as a gonad stimulant, is a type of drug which increases the secretion of one or both of the major gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH).^[1] This, in turn, results in increased function and maintenance of the gonads and increased gonadal steroidogenesis of sex hormones such as androgens, estrogens, and progestogens. Progonadotropins are the functional opposites of antigonadotropins. They have clinical applications in the treatment of hypogonadism and infertility.^[2] Conversely, hypergonadotropic effects can occur as a side effect of some drugs. Examples of progonadotropic drugs include gonadotropin-releasing hormone (GnRH) agonists when administered in a pulsatile (as opposed to continuous) manner, antiestrogens such as tamoxifen, clomifene, fulvestrant, and aromatase inhibitors like anastrozole,^[2] and, only in men, pure antiandrogens such as flutamide, bicalutamide, enzalutamide, and apalutamide.^[3]

References

^ Cole, H. H. (1975). "Studies on Reproduction with Emphasis on Gonadotropins, Antigonadotropins and Progonadotropins". Biology of Reproduction. 12 (2): 194–211. doi:10.1095/biolreprod12.2.194. ISSN 0006-3363. PMID 1122329.
^ ^a ^b Vandekerckhove P, Lilford R, Vail A, Hughes E (2000). "Clomiphene or tamoxifen for idiopathic oligo/asthenospermia". Cochrane Database Syst Rev (2): CD000151. doi:10.1002/14651858.CD000151. PMC 10865959. PMID 10796497. (Retracted)
^ Perdonà, Sisto; Autorino, Riccardo; De Placido, Sabino; D'Armiento, Massimo; Gallo, Antonio; Damiano, Rocco; Pingitore, Domenico; Gallo, Luigi; De Sio, Marco; Bianco, Angelo Raffaele; Di Lorenzo, Giuseppe (2005). "Efficacy of tamoxifen and radiotherapy for prevention and treatment of gynaecomastia and breast pain caused by bicalutamide in prostate cancer: a randomised controlled trial". The Lancet Oncology. 6 (5): 295–300. doi:10.1016/S1470-2045(05)70103-0. ISSN 1470-2045. PMID 15863377.

GnRHTooltip Gonadotropin-releasing hormone and gonadotropins

GnRH modulators
(incl. analogues)

Agonists	Peptide: Azagly-nafarelin Buserelin Deslorelin Fertirelin Gonadorelin Goserelin Histrelin Lecirelin Leuprorelin (leuprolide) Nafarelin Peforelin Triptorelin
Antagonists	Peptide: Abarelix Cetrorelix Degarelix Ganirelix Non-peptide: Elagolix Linzagolix^† Relugolix (+estradiol/norethisterone acetate)

Preparations	Follicle-stimulating hormone Human chorionic gonadotropin Luteinizing hormone Menotropin Urofollitropin

Others
(indirect)

Progonadotropins	Sex steroid antagonists (via disinhibition of the HPG axis): Antiandrogens (e.g., flutamide, bicalutamide, enzalutamide) Antiestrogens/SERMsTooltip Selective estrogen receptor modulators (e.g., tamoxifen, clomifene, enclomifene) Aromatase inhibitors (e.g., anastrozole) GnRH agonists (e.g., GnRHTooltip gonadotropin-releasing hormone)
Antigonadotropins	Sex steroid agonists (via negative feedback on the HPG axis): Androgens/anabolic steroids (e.g., testosterone, nandrolone esters, oxandrolone) D₂ receptor antagonists (prolactin releasers) (incl., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, sulpiride) Estrogens (incl., bifluranol, estradiol, estradiol esters, ethinylestradiol, diethylstilbestrol, paroxypropione) Progestogens (incl. progestins, e.g., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone caproate, gestonorone caproate, medroxyprogesterone acetate, megestrol acetate) Others (mixed or unknown mechanism of action): Danazol Gestrinone Metallibure

Progonadotropins

Sex steroid antagonists (via disinhibition of the HPG axis): Antiandrogens (e.g., flutamide, bicalutamide, enzalutamide)
Antiestrogens/SERMsTooltip Selective estrogen receptor modulators (e.g., tamoxifen, clomifene, enclomifene)
Aromatase inhibitors (e.g., anastrozole)
GnRH agonists (e.g., GnRHTooltip gonadotropin-releasing hormone)

See also: GnRH and gonadotropin receptor modulators; Androgens and antiandrogens; Estrogens and antiestrogens; Progestogens and antiprogestogens

GnRHTooltip Gonadotropin-releasing hormone receptor and gonadotropin receptor modulators

GnRHTooltip Gonadotropin-releasing hormone receptor

LH/hCGTooltip Luteinizing hormone/choriogonadotropin receptor	Agonists: Peptides: Choriogonadotropin alfa Human chorionic gonadotropin Luteinizing hormone Lutropin alfa Menotropin (human menopausal gonadotropin)
FSHTooltip Follicle-stimulating hormone receptor	Agonists: Peptides: Corifollitropin alfa Follicle-stimulating hormone Follitropin alfa Follitropin beta Follitropin epsilon Menotropin (human menopausal gonadotropin) Urofollitropin Varfollitropin alfa NAMs: Non-peptides: ADX-61623