Linzagolix, sold under the brand name Yselty, is a

medication A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the medical field an ...

used in the treatment of uterine fibroids.https://www.ema.europa.eu/en/documents/product-information/yselty-epar-product-information_en.pdf Linzagolix is a

small-molecule Within the fields of molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs ar ...

, non-peptide,

orally active Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are in ...

gonadotropin-releasing hormone antagonist (GnRH antagonist) developed by Kissei Pharmaceutical and ObsEva. In June 2022, it was approved for medical use in the European Union and in the United Kingdom.

Medical uses

Linzagolix is indicated for treatment of moderate to severe symptoms of uterine fibroids in adult women of reproductive age.

Available forms

Linzagolix is available as linzagolix choline, the

choline Choline is an essential nutrient for humans and many other animals. Choline occurs as a cation that forms various salts (X− in the depicted formula is an undefined counteranion). Humans are capable of some ''de novo synthesis'' of choline but ...

salt Salt is a mineral composed primarily of sodium chloride (NaCl), a chemical compound belonging to the larger class of salts; salt in the form of a natural crystalline mineral is known as rock salt or halite. Salt is present in vast quanti ...

of linzagolix, in the form of 100 and 200mg

film-coated A film coating is a thin polymer-based coat that is typically sprayed on to a solid pharmaceutical dosage form, such as a tablet, capsule, pellet or granule. Film coating can impact both its appearance and its pharmacokinetics making it an ess ...

oral tablets.

Pharmacology

Pharmacodynamics

Linzagolix acts as a selective antagonist of the GnRH receptor, the

biological target A biological target is anything within a living organism to which some other entity (like an endogenous ligand or a drug) is directed and/or binds, resulting in a change in its behavior or function. Examples of common classes of biological targets ...

of GnRH. By blocking this receptor, linzagolix prevents GnRH-mediated

secretion 440px Secretion is the movement of material from one point to another, such as a secreted chemical substance from a cell or gland. In contrast, excretion is the removal of certain substances or waste products from a cell or organism. The classica ...

of the

gonadotropin Gonadotropins are glycoprotein hormones secreted by gonadotropic cells of the anterior pituitary of vertebrates. This family includes the mammalian hormones follicle-stimulating hormone (FSH) and luteinizing hormone (LH), the placental/ chori ...

luteinizing hormone Luteinizing hormone (LH, also known as luteinising hormone, lutropin and sometimes lutrophin) is a hormone produced by gonadotropic cells in the anterior pituitary gland. The production of LH is regulated by gonadotropin-releasing hormone (Gn ...

(LH) and

follicle-stimulating hormone Follicle-stimulating hormone (FSH) is a gonadotropin, a glycoprotein polypeptide hormone. FSH is synthesized and secreted by the gonadotropic cells of the anterior pituitary gland and regulates the development, growth, pubertal maturation, ...

(FSH), and prevents them from signaling the

gonad A gonad, sex gland, or reproductive gland is a mixed gland that produces the gametes and sex hormones of an organism. Female reproductive cells are egg cells, and male reproductive cells are sperm. The male gonad, the testicle, produces ...

s to produce

sex hormone Sex hormones, also known as sex steroids, gonadocorticoids and gonadal steroids, are steroid hormones that interact with vertebrate steroid hormone receptors. The sex hormones include the androgens, estrogens, and progestogens. Their effects ...

s including

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 a ...

progesterone Progesterone (P4) is an endogenous steroid and progestogen sex hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. It belongs to a group of steroid hormones called the progestogens and is the ma ...

, and

androgen An androgen (from Greek ''andr-'', the stem of the word meaning "man") is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This in ...

s. In clinical studies, linzagolix fully suppressed estradiol levels (median <20pg/mL) in women at a dosage of 200mg/day, whereas partial suppression of estradiol levels (median 20–60pg/mL) occurred at a dosage 100mg/day. Progesterone levels were also variably suppressed with these dosages.

Pharmacokinetics

The elimination half-life of linzagolix with repeated administration is approximately 15hours.

History

On 16 December 2021, and on 22 April 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Yselty, intended for the treatment of symptoms of uterine fibroids. The applicant for this medicinal product is ObsEva Ireland Ltd. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Approval for use in this indication in the EU was granted in June 2022.

Society and culture

Brand names

Linzagolix is sold under the brand name Yselty.

Availability

Linzagolix is available in the European Union and in the United Kingdom.

References

External links

* * {{Portal bar , Medicine Carboxylic acids Ethers Fluoroarenes GnRH antagonists Pyrimidines