Ormeloxifene, also known as centchroman, is one of the

selective estrogen receptor modulator Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs), are a class of drugs that act on the estrogen receptor (ER). A characteristic that distinguishes these substances from pure ER agonists a ...

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

estrogen receptor Estrogen receptors (ERs) are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen ( 17β-estradiol). Two classes of ER exist: nuclear estrogen receptors (ERα and ERβ), which are members of the ...

. 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 mod ...

oral contraceptive Oral contraceptives, abbreviated OCPs, also known as birth control pills, are medications taken by mouth for the purpose of birth control. Female Two types of female oral contraceptive pill, taken once per day, are widely available: * The combi ...

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 unwanted pregnancy. Birth control has been used since ancient times, but effective and safe methods of birth contr ...

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 Novex-DS, Centron, and Sevista.

Medical uses

Ormeloxifene is primarily used as a contraceptive but may also be effective for

dysfunctional uterine bleeding Abnormal uterine bleeding (AUB), also known as (AVB) or as atypical vaginal bleeding, is vaginal bleeding from the uterus that is abnormally frequent, lasts excessively long, is heavier than normal, or is irregular. The term dysfunctional uterin ...

and advanced

breast cancer Breast cancer is cancer that develops from breast tissue. Signs of breast cancer may include a lump in the breast, a change in breast shape, dimpling of the skin, milk rejection, fluid coming from the nipple, a newly inverted nipple, or a re ...

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 taken orally by women. The pill contains two important hormones: progest ...

Other indications

* Ormeloxifene has also been tested in experimental setting as a treatment for

menorrhagia Heavy menstrual bleeding (HMB), previously known as menorrhagia or hypermenorrhea, is a menstrual period with excessively heavy flow. It is a type of abnormal uterine bleeding Abnormal uterine bleeding (AUB), also known as (AVB) or as atypical ...

. * use in treatment of

mastalgia Breast pain is the symptom of discomfort in either one or both breasts. Pain in both breasts is often described as ''breast tenderness'', is usually associated with the menstrual period and is not serious. Pain that involves only one part of a br ...

and

fibroadenoma Fibroadenomas are benign breast tumours characterized by an admixture of stromal and epithelial tissue. Breasts are made of lobules (milk producing glands) and ducts (tubes that carry the milk to the nipple). These are surrounded by glandula ...

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 or oestrogen is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal acti ...

ic (e.g.,

bone A bone is a Stiffness, rigid Organ (biology), organ that constitutes part of the skeleton in most vertebrate animals. Bones protect the various other organs of the body, produce red blood cell, red and white blood cells, store minerals, provid ...

s), in other parts of the body, its action is

antiestrogen Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body. They act by blocking the estrogen receptor (ER) and/or ...

ic (e.g.,

uterus The uterus (from Latin ''uterus'', plural ''uteri'') or womb () is the organ in the reproductive system of most female mammals, including humans that accommodates the embryonic and fetal development of one or more embryos until birth. The uter ...

breast The breast is one of two prominences located on the upper ventral region of a primate's torso. Both females and males develop breasts from the same embryological tissues. In females, it serves as the mammary gland, which produces and secret ...

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 make pregnancy possible. The ovarian cycle controls the production and release of eggs a ...

between

ovulation Ovulation is the release of eggs from the ovaries. In women, this event occurs when the ovarian follicles rupture and release the secondary oocyte ovarian cells. After ovulation, during the luteal phase, the egg will be available to be fertilized ...

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 (singular salpinx), are paired tubes in the human female that stretch from the uterus to the ovaries. The fallopian tubes are part of the female reproductive system. In ot ...

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 capital and the largest city of the Indian state of Uttar Pradesh and it is also the second largest urban agglomeration in Uttar Pradesh. Lucknow is the administrative headquarters of the eponymous district and division ...

, 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, primarily its western or right bank, Delhi shares borders w ...

in July 1991 and in

India India, officially the Republic of India (Hindi: ), is a country in South Asia. It is the seventh-largest country by area, the second-most populous country, and the most populous democracy in the world. Bounded by the Indian Ocean on the so ...

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 Torrent Pharmaceuticals Ltd is an Indian multinational pharmaceutical company, owned by Torrent Group and headquartered in Ahmedabad. It was promoted by U. N. Mehta, initially as Trinity Laboratories Ltd, and was later renamed Torrent Pharmac ...

, 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 journal articles and books in the life sciences. It serves as a thesaurus that facilitates searching. Created and updated by the United States N ...

(MeSH) database
Reproductive Health Online
a

Johns Hopkins University Johns Hopkins University (Johns Hopkins, Hopkins, or JHU) is a private university, private research university in Baltimore, Maryland. Founded in 1876, Johns Hopkins is the oldest research university in the United States and in the western hem ...

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 Pyrrolidines Selective estrogen receptor modulators