Ormeloxifene, also known as centchroman, is one of the

selective estrogen receptor modulator Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonists/antagonists (ERAAs), are a class of drugs that act on estrogen receptors (ERs). Compared to pure ER agonists–antagonists (e.g., full agonists and silent ...

s, or SERMs, a class of medication which acts on the

estrogen receptor Estrogen receptors (ERs) are proteins found in cell (biology), cells that function as receptor (biochemistry), receptors for the hormone estrogen (17β-estradiol). There are two main classes of ERs. The first includes the intracellular estrogen ...

. It is best known as a

nonsteroidal A nonsteroidal compound is a drug that is not a steroid nor a steroid derivative. Nonsteroidal anti-inflammatory drugs (NSAIDs) are distinguished from corticosteroids as a class of anti-inflammatory agents. List of nonsteroidal steroid receptor mo ...

oral contraceptive which is taken once per week. In India, ormeloxifene has been available as

birth control Birth control, also known as contraception, anticonception, and fertility control, is the use of methods or devices to prevent pregnancy. Birth control has been used since ancient times, but effective and safe methods of birth control only be ...

since the early 1990s, and it was marketed there under the trade name Saheli, currently available free-of-cost for the women in India as Chhaya (Centchroman). 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 Breast cancer is a cancer that develops from breast tissue. Signs of breast cancer may include a Breast lump, lump in the breast, a change in breast shape, dimpling of the skin, Milk-rejection sign, milk rejection, fluid coming from the nipp ...

Birth control

Ormeloxifene may be used as a weekly oral contraceptive. 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. From the thirteenth week on, it is taken once per week. 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%. It has a failure rate of about 1-2% with ideal use which is slightly less effective than found for

combined oral contraceptive pill The combined oral contraceptive pill (COCP), often referred to as the birth control pill or colloquially as "the pill", is a type of birth control that is designed to be Oral administration, taken orally by women. It is the oral form of combi ...

Other indications

* Ormeloxifene has also been tested in experimental setting as a treatment for menorrhagia. * use in treatment of mastalgia and fibroadenoma has also been described.

Side effects

There are concerns that ormeloxifene may cause delayed menstruation.

Pharmacology

Ormeloxifene is a

(SERM). In some parts of the body, its action is

estrogen Estrogen (also spelled oestrogen in British English; see spelling differences) is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three ...

ic (e.g.,

bone A bone is a rigid organ that constitutes part of the skeleton in most vertebrate animals. Bones protect the various other organs of the body, produce red and white blood cells, store minerals, provide structure and support for the body, ...

s), in other parts of the body, its action is antiestrogenic (e.g.,

uterus The uterus (from Latin ''uterus'', : uteri or uteruses) or womb () is the hollow organ, organ in the reproductive system of most female mammals, including humans, that accommodates the embryonic development, embryonic and prenatal development, f ...

breast The breasts are two prominences located on the upper ventral region of the torso among humans and other primates. Both sexes develop breasts from the same embryology, embryological tissues. The relative size and development of the breasts is ...

s). It causes an asynchrony in the

menstrual cycle The menstrual cycle is a series of natural changes in hormone production and the structures of the uterus and ovaries of the female reproductive system that makes pregnancy possible. The ovarian cycle controls the production and release of eg ...

between

ovulation Ovulation is an important part of the menstrual cycle in female vertebrates where the egg cells are released from the ovaries as part of the ovarian cycle. In female humans ovulation typically occurs near the midpoint in the menstrual cycle and ...

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, 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 tube The fallopian tubes, also known as uterine tubes, oviducts or salpinges (: salpinx), are paired tubular sex organs in the human female body that stretch from the Ovary, ovaries to the uterus. The fallopian tubes are part of the female reproduct ...

s more quickly than is normal. Presumably, this combination of effects creates an environment such that if fertilization occurs, implantation will not be possible.

History

Ormeloxifene was first discovered by Central Drug Research Institute (CDRI) in

Lucknow Lucknow () is the List of state and union territory capitals in India, capital and the largest city of the List of state and union territory capitals in India, Indian state of Uttar Pradesh and it is the administrative headquarters of the epon ...

, India. Ormeloxifene was marketed in

Delhi Delhi, officially the National Capital Territory (NCT) of Delhi, is a city and a union territory of India containing New Delhi, the capital of India. Straddling the Yamuna river, but spread chiefly to the west, or beyond its Bank (geography ...

in July 1991 and in

India India, officially the Republic of India, is a country in South Asia. It is the List of countries and dependencies by area, seventh-largest country by area; the List of countries by population (United Nations), most populous country since ...

in 1992, under the brand names ''Saheli'' and ''Choice-7''. Since 2018, Centchroman is provided free-of-cost to the women in India by the government under the brand name ''Chhaya''.

Society and culture

Marketing

As of 2009, ormeloxifene was legally available only in India. 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

External links

United States National Library of Medicine
''Centchroman'' entry in the

Medical Subject Headings Medical Subject Headings (MeSH) is a comprehensive controlled vocabulary for the purpose of indexing Academic journal, journal articles and books in the Life science, life sciences. It serves as a thesaurus of index terms that facilitates searc ...

(MeSH) database
Reproductive Health Online
a

Johns Hopkins University The Johns Hopkins University (often abbreviated as Johns Hopkins, Hopkins, or JHU) is a private university, private research university in Baltimore, Maryland, United States. Founded in 1876 based on the European research institution model, J ...

affiliate providing information on Centchroman
Central Drug Research Institute
, Lucknow,

: 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. {{Estrogen receptor modulators Chromanes Drugs acting on the genito-urinary system Hormonal contraception Phenol ethers 1-Pyrrolidinyl compounds Selective estrogen receptor modulators