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Ormeloxifene
Ormeloxifene
Background
Type	Antiestrogen
First use	1991
Failure rates (first year)
Perfect use	2%
Typical use	9%
Usage
Duration effect	One week
Reversibility	Immediate
User reminders	Taken twice weekly for first 13 weeks
Clinic review	Annually
Advantages and disadvantages
STI protection	No
Periods	May disrupt
Safe while breastfeeding	Yes
Weight	No proven effect
Benefits	Non hormonal
Risks	Delayed menstruation
Medical notes
	Only approved as a contraceptive in India

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;
CAS Number	31477-60-8 ;
PubChem CID	154413;
ChemSpider	32935 ;
UNII	44AXY5VE90;
KEGG	D08301 ;
ChEMBL	ChEMBL301327 ;
Chemical and physical data
Formula	C30H35NO3
Molar mass	457.614 g·mol−1
3D model (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 ; Key:XZEUAXYWNKYKPL-URLMMPGGSA-N ;
	(what is this?) (verify)

Ormeloxifene, also known as centchroman, is one of the selective estrogen receptor modulators,^[2] or SERMs, a class of medication which acts on the estrogen receptor. It is best known as a nonsteroidal oral contraceptive which is taken once per week. In India, ormeloxifene has been available as birth control since the early 1990s, and it was marketed there under the trade name Saheli,^[3] currently available free-of-cost for the women in India as Chhaya (Centchroman).^[4]^[5]

Ormeloxifene has also been licensed under the trade names Ormalin, Novex-DS, Centron, and Sevista.

Medical uses

Ormeloxifene is primarily used as a contraceptive but may also be effective for dysfunctional uterine bleeding and advanced breast cancer.^[6]

Birth control

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]

Side effects

There are concerns that ormeloxifene may cause delayed menstruation.^[12]

Pharmacology

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.

References

^ Gupta RC, Paliwal JK, Nityanand S, Asthana OP, Lal J (November 1995). "Centchroman: a new non-steroidal oral contraceptive in human milk". Contraception. 52 (5): 301–305. doi:10.1016/0010-7824(95)00214-U. PMID 8585887.
^ Makker A, Tandon I, Goel MM, Singh M, Singh MM (June 2009). "Effect of ormeloxifene, a selective estrogen receptor modulator, on biomarkers of endometrial receptivity and pinopode development and its relation to fertility and infertility in Indian subjects". Fertility and Sterility. 91 (6): 2298–2307. doi:10.1016/j.fertnstert.2008.04.018. PMID 18675966.
^ "HLL - Product Overview". Archived from the original on 1 November 2018.
^ ^a ^b "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 from the original on 11 May 2021. Retrieved 29 June 2020.
^ "Contraception and women's empowerment: Here's how safe, reliable contraceptives are freeing women to earn". Hindustan Times. 10 July 2018. Retrieved 29 June 2020.
^ ^a ^b ^c ^d Lal J (April 2010). "Clinical pharmacokinetics and interaction of centchroman--a mini review". Contraception. 81 (4): 275–280. doi:10.1016/j.contraception.2009.11.007. PMID 20227542.
^ "Home | ReproLinePlus".
^ 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. PMID 11257249.
^ ^a ^b ^c ^d ^e Singh 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. PMID 11410933. S2CID 37474826.
^ 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. PMID 19751337. S2CID 39172838.
^ Dhar A, Srivastava A (June 2007). "Role of centchroman in regression of mastalgia and fibroadenoma". World Journal of Surgery. 31 (6): 1178–1184. doi:10.1007/s00268-007-9040-4. PMID 17431715. S2CID 22828570.
^ Shelly W, Draper MW, Krishnan V, Wong M, Jaffe RB (March 2008). "Selective estrogen receptor modulators: an update on recent clinical findings". Obstetrical & Gynecological Survey. 63 (3): 163–181. doi:10.1097/OGX.0b013e31816400d7. PMID 18279543. S2CID 23585991.
^ ^a ^b "CSIR-CDRI | Home". cdri.res.in. Retrieved 29 June 2020.
^ 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. PMID 18279897.
^ "Centchroman". CSIR-CDRI. Archived from the original on 14 February 2019. Retrieved 25 September 2018.
^ Lal J (April 2010). "Clinical pharmacokinetics and interaction of centchroman--a mini review". Contraception. 81 (4): 275–280. doi:10.1016/j.contraception.2009.11.007. PMID 20227542.
^ "परिवार नियोजन विधियों में छाया से अधिक अंतरा में बढ़ी महिलाओं की दिलचस्पी, जानिये इनके बारे में". Patrika News (in Hindi). 22 May 2018. Retrieved 29 June 2020.
^ Bhatia I (7 April 2018). "antara chhaya: Two months after launch, Antara, Chhaya contraceptives get good response from locals". The Times of India. Retrieved 29 June 2020.
^ Shelar J (12 January 2018). "BMC rolls out new contraceptive pill". The Hindu. ISSN 0971-751X. Retrieved 29 June 2020.
^ Tribhuwan RD, Patil BD (2009). Body image : human reproduction and birth control : a tribal perspective. New Delhi: Discovery Pub. House. p. 20. ISBN 978-81-8356-388-8.

External links

United States National Library of Medicine Centchroman entry in the Medical Subject Headings (MeSH) database
Reproductive Health Online, a Johns Hopkins University affiliate providing information on Centchroman
Central Drug Research Institute Archived 5 August 2016 at the Wayback Machine, Lucknow, India: a government-funded laboratory, conducting R&D on Centchroman as birth control.
Ministry of Health and Family Welfare - Indian government site; information about availability of Saheli.

[1] Gupta RC, Paliwal JK, Nityanand S, Asthana OP, Lal J (November 1995). "Centchroman: a new non-steroidal oral contraceptive in human milk". Contraception. 52 (5): 301–305. doi:10.1016/0010-7824(95)00214-U. PMID 8585887.

[pmid18675966-2] Makker A, Tandon I, Goel MM, Singh M, Singh MM (June 2009). "Effect of ormeloxifene, a selective estrogen receptor modulator, on biomarkers of endometrial receptivity and pinopode development and its relation to fertility and infertility in Indian subjects". Fertility and Sterility. 91 (6): 2298–2307. doi:10.1016/j.fertnstert.2008.04.018. PMID 18675966.

[3] "HLL - Product Overview". Archived from the original on 1 November 2018.

[humdo.nhp.gov.in-4] "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 from the original on 11 May 2021. Retrieved 29 June 2020.

[5] "Contraception and women's empowerment: Here's how safe, reliable contraceptives are freeing women to earn". Hindustan Times. 10 July 2018. Retrieved 29 June 2020.

[Review10-6] Lal J (April 2010). "Clinical pharmacokinetics and interaction of centchroman--a mini review". Contraception. 81 (4): 275–280. doi:10.1016/j.contraception.2009.11.007. PMID 20227542.

[7] "Home | ReproLinePlus".

[pmid11257249-8] 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. PMID 11257249.

[Singh_2001-9] Singh 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. PMID 11410933. S2CID 37474826.

[pmid19751337-10] 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. PMID 19751337. S2CID 39172838.

[pmid17431715-11] Dhar A, Srivastava A (June 2007). "Role of centchroman in regression of mastalgia and fibroadenoma". World Journal of Surgery. 31 (6): 1178–1184. doi:10.1007/s00268-007-9040-4. PMID 17431715. S2CID 22828570.

[12] Shelly W, Draper MW, Krishnan V, Wong M, Jaffe RB (March 2008). "Selective estrogen receptor modulators: an update on recent clinical findings". Obstetrical & Gynecological Survey. 63 (3): 163–181. doi:10.1097/OGX.0b013e31816400d7. PMID 18279543. S2CID 23585991.

[cdri.res.in-13] "CSIR-CDRI | Home". cdri.res.in. Retrieved 29 June 2020.

[14] 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.

[pmid18279897-15] 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. PMID 18279897.

[16] "Centchroman". CSIR-CDRI. Archived from the original on 14 February 2019. Retrieved 25 September 2018.

[pmid20227542-17] Lal J (April 2010). "Clinical pharmacokinetics and interaction of centchroman--a mini review". Contraception. 81 (4): 275–280. doi:10.1016/j.contraception.2009.11.007. PMID 20227542.

[Patrika_News_2018-18] "परिवार नियोजन विधियों में छाया से अधिक अंतरा में बढ़ी महिलाओं की दिलचस्पी, जानिये इनके बारे में". Patrika News (in Hindi). 22 May 2018. Retrieved 29 June 2020.

[Bhatia_2018-19] Bhatia I (7 April 2018). "antara chhaya: Two months after launch, Antara, Chhaya contraceptives get good response from locals". The Times of India. Retrieved 29 June 2020.

[Shelar_2018-20] Shelar J (12 January 2018). "BMC rolls out new contraceptive pill". The Hindu. ISSN 0971-751X. Retrieved 29 June 2020.

[21] Tribhuwan RD, Patil BD (2009). Body image : human reproduction and birth control : a tribal perspective. New Delhi: Discovery Pub. House. p. 20. ISBN 978-81-8356-388-8.

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PROFILPELAJAR.COM

Ormeloxifene

Medical uses

Birth control

Other indications

Side effects

Pharmacology

History

Society and culture

Marketing

See also

References

Further reading

External links

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