Opigolix

Short description: Chemical compound

Opigolix

Clinical data
Other names| ASP-1707
Routes of
administration| By mouth
Drug class| GnRH modulator; GnRH antagonist; Antigonadotropin
Identifiers

IUPAC name

* (2R)-N'-[5-[3-(2,5-difluorophenyl)-2-(1,3-dihydrobenzimidazol-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl]sulfonyl-2-hydroxypropanimidamide

CAS Number|

* 912587-25-8 Y

PubChem CID|

* 11977994

UNII|

* VQ6CK0CITA

KEGG|

* D11351

Chemical and physical data
Formula| C25H19F3N4O5S
Molar mass| 544.51 g·mol−1
3D model (JSmol)|

* Interactive image

SMILES

* C[C@@H](O)/C(N)=N/S(=O)(=O)c1cc(C(=O)C(C(=O)c2cc(F)ccc2F)=C2Nc3ccccc3N2)ccc1F

InChI

* InChI=1S/C25H19F3N4O5S/c1-12(33)24(29)32-38(36,37)20-10-13(6-8-17(20)28)22(34)21(23(35)15-11-14(26)7-9-16(15)27)25-30-18-4-2-3-5-19(18)31-25/h2-12,30-31,33H,1H3,(H2,29,32)/t12-/m1/s1

* Key:CWNLBPBIFALUQD-GFCCVEGCSA-N

Opigolix (INN, USAN; developmental code name ASP-1707) is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) which was under development by Astellas Pharma for the treatment of endometriosis and rheumatoid arthritis.[1][2] It was also under investigation for the treatment of prostate cancer.[1] It reached phase II clinical trials for both endometriosis and rheumatoid arthritis prior to the discontinuation of its development in April 2018.[1]

## See also

* Gonadotropin-releasing hormone receptor § Antagonists

## References

1. ↑ 1.0 1.1 1.2 "Opigolix - Astellas Pharma - AdisInsight". http://adisinsight.springer.com/drugs/800032657.
2. ↑ "Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain". Women's Health 11 (1): 19–28. 2015. doi:10.2217/whe.14.68. PMID 25581052.

## External links

* Opigolix - AdisInsight

* v
* t
* e

GnRH 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†

Gonadotropins|

| 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/SERMs (e.g., tamoxifen, Chemistry:Clomifene

|

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)
* Progestogen|Progestogens (incl. progestins, e.g., Chemistry:Chlormadinone acetate

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

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

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Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:Opigolix&oldid=492655"
*[CID]: Compound ID
*[INN]: International Nonproprietary Name
*[USAN]: United States Adopted Name
*[v]: View this template
*[t]: Discuss this template
*[e]: Edit this template
*[GnRH]: gonadotropin-releasing hormone
*[HPG]: hypothalamic–pituitary–gonadal
*[SERMs]: Selective estrogen receptor modulators