Ormeloxifene, also known ascentchroman, is one of theselective estrogen receptor modulators,[2] or SERMs, a class of medication which acts on theestrogen receptor. It is best known as anonsteroidaloral contraceptive which is taken once per week. In India, ormeloxifene has been available asbirth control since the early 1990s, and it was marketed there under the trade nameSaheli,[3] currently available free-of-cost for the women in India asChhaya (Centchroman).[4][5]
Ormeloxifene has also been licensed under the trade namesOrmalin,Novex-DS,Centron, andSevista.
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.[citation needed]
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]
Ormeloxifene is aselective estrogen receptor modulator (SERM). In some parts of the body, its action isestrogenic (e.g.,bones), in other parts of the body, its action isantiestrogenic (e.g.,uterus,breasts).[13][14][15] It causes an asynchrony in themenstrual cycle betweenovulation 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 thefallopian 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]
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.[citation needed]
manufactured byTorrent Pharmaceuticals, and marketed as birth control under the trade nameCentron. Centron was discontinued.
A new license for ormeloxifene was issued toHindustan Latex Ltd., which now manufactures ormeloxifene as birth control under the trade namesSaheli,Novex, andNovex-DS.
Torrent Pharmaceuticals has resumed manufacture of ormeloxifene under the trade nameSevista, as a treatment for dysfunctional uterine bleeding.
^ab"Chhaya".Centre for Health Informatics (CHI) of the National Health Portal (NHP), by the Ministry of Health and Family Welfare (MoHFW). Government of India. Archived fromthe original on 11 May 2021. Retrieved29 June 2020.
^Lal J, Nitynand S, Asthana OP, Nagaraja NV, Gupta RC (January 2001). "Optimization of contraceptive dosage regimen of Centchroman".Contraception.63 (1):47–51.doi:10.1016/S0010-7824(00)00189-X.PMID11257249.
^abcdeSingh MM (July 2001). "Centchroman, a selective estrogen receptor modulator, as a contraceptive and for the management of hormone-related clinical disorders".Medicinal Research Reviews.21 (4):302–347.doi:10.1002/med.1011.PMID11410933.S2CID37474826.
^Kriplani A, Kulshrestha V, Agarwal N (August 2009). "Efficacy and safety of ormeloxifene in management of menorrhagia: a pilot study".The Journal of Obstetrics and Gynaecology Research.35 (4):746–752.doi:10.1111/j.1447-0756.2008.00987.x.PMID19751337.S2CID39172838.
^Kumar GR, Rituraj K, Hemant BK, Singh MM (November 2007).In-vitro anti-cancer breast activity of ormeloxifene is mediated via induction of apoptosis and autophagy. 37th annual conference of the endocrine society of India. Vol. 30. p. 35.
^Nigam M, Ranjan V, Srivastava S, Sharma R, Balapure AK (March 2008). "Centchroman induces G0/G1 arrest and caspase-dependent apoptosis involving mitochondrial membrane depolarization in MCF-7 and MDA MB-231 human breast cancer cells".Life Sciences.82 (11–12):577–590.doi:10.1016/j.lfs.2007.11.028.PMID18279897.
Ray S, Grover PK, Kamboj VP, Setty BS, Kar AB, Anand N (February 1976). "Antifertility agents. 12. Structure-activity relationship of 3,4-diphenylchromenes and -chromans".Journal of Medicinal Chemistry.19 (2):276–279.doi:10.1021/jm00224a014.PMID1249807.
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