Ormeloxifene

Ormeloxifene

Clinical data
Trade names	Centron, Novex-DS, Saheli, Sevista, Chhaya
Other names	Centchroman
Routes of administration	By mouth
Drug class	Selective estrogen receptor modulator
ATC code	G03XC04 (WHO)
Legal status
Legal status	US: Not FDA approved Rx-only in India
Pharmacokinetic data
Elimination half-life	7 days
Identifiers
IUPAC name 1-[2-[4-[(3S,4S)-7-methoxy-2,2-dimethyl-3-phenyl-chroman-4-yl]phenoxy]ethyl]pyrrolidine
JSmol)	Interactive image
SMILES CC1([C@@H]([C@H](c2ccc(cc2O1)OC)c3ccc(cc3)OCCN4CCCC4)c5ccccc5)C
InChI InChI=1S/C30H35NO3/c1-30(2)29(23-9-5-4-6-10-23)28(26-16-15-25(32-3)21-27(26)34-30)22-11-13-24(14-12-22)33-20-19-31-17-7-8-18-31/h4-6,9-16,21,28-29H,7-8,17-20H2,1-3H3/t28-,29+/m0/s1 N Key:XZEUAXYWNKYKPL-URLMMPGGSA-N N
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Ormeloxifene, also known as centchroman, is one of the

Ormeloxifene may be used as a weekly oral contraceptive.[6] The weekly schedule is an advantage for women who prefer an oral contraceptive, but find it difficult or impractical to adhere to a daily schedule required by other oral contraceptives.

For the first twelve weeks of use, it is advised to take the ormeloxifene pill twice per week.^[6] From the thirteenth week on, it is taken once per week.^[6][7] The consensus is that backup protection in the first month is a cautious but sensible choice. A standard dose is 30 mg weekly, but 60 mg loading doses can reduce pregnancy rates by 38%.^[8]

It has a failure rate of about 1-2% with ideal use which is slightly less effective than found for combined oral contraceptive pills.^[9]

Other indications

• Ormeloxifene has also been tested in experimental setting as a treatment for
  menorrhagia.^[10]
• use in treatment of
  mastalgia and fibroadenoma has also been described.^[11]

Ormeloxifene is a selective estrogen receptor modulator (SERM). In some parts of the body, its action is estrogenic (e.g., bones), in other parts of the body, its action is antiestrogenic (e.g., uterus, breasts).^[13][14][15] It causes an asynchrony in the menstrual cycle between ovulation and the development of the uterine lining, although its exact mode of action is not well defined. In clinical trials, it caused ovulation to occur later than it normally would in some women,^[9] but did not affect ovulation in the majority of women, while causing the lining of the uterus to build more slowly. It speeds the transport of any fertilized egg through the fallopian tubes more quickly than is normal.^[9] Presumably, this combination of effects creates an environment such that if fertilization occurs, implantation will not be possible.^[9]

History

Ormeloxifene was first discovered by Central Drug Research Institute (CDRI) in Lucknow, India.^[13][16] Ormeloxifene was marketed in Delhi in July 1991 and in India in 1992, under the brand names Saheli and Choice-7.^[9][17]

Since 2018, Centchroman is provided free-of-cost to the women in India by the government under the brand name Chhaya.^{[4][18][19][20]}

Society and culture

Marketing

As of 2009, ormeloxifene was legally available only in India.^[21]

Ormeloxifene has been tested and licensed as a form of birth control, as well as a treatment for dysfunctional uterine bleeding.

• manufactured by Torrent Pharmaceuticals, and marketed as birth control under the trade name Centron. Centron was discontinued.
• A new license for ormeloxifene was issued to Hindustan Latex Ltd., which now manufactures ormeloxifene as birth control under the trade names Saheli, Novex, and Novex-DS.
• Torrent Pharmaceuticals has resumed manufacture of ormeloxifene under the trade name Sevista, as a treatment for dysfunctional uterine bleeding.

See also

• Levormeloxifene

References