A selective estrogen receptor degrader or downregulator (SERD) is a type of
drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
which binds to the
estrogen receptor (ER) and, in the process of doing so, causes the ER to be degraded and thus
downregulated.
They are used to treat estrogen receptor-sensitive or progesterone receptor-sensitive
breast cancer, along with older classes of drugs like
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 (SERMs) and
aromatase inhibitors.
[
As of 2016 the only marketed SERD was fulvestrant (brand name ]Faslodex
Fulvestrant, sold under the brand name Faslodex among others, is a medication used to treat hormone receptor (HR)-positive metastatic breast cancer in postmenopausal women with disease progression as well as HR-positive, HER2-negative advanced b ...
).brilanestrant
Brilanestrant (INN) (developmental code names GDC-0810, ARN-810, RG-6046, RO-7056118) is a nonsteroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was discovered by Aragon Pharmaceu ...
and elacestrant.selective androgen receptor degrader
A selective androgen receptor degrader or downregulator (SARD) is a type of pharmaceutical drug, drug which interacts with the androgen receptor (AR) such that it causes the AR to be degraded and thus downregulation and upregulation, downregulate ...
s (SARDs).[
]
Investigational
Fulvestrant requires large-volume and frequently painful intramuscular injections. In response, pharmaceutical companies are currently developing oral SERDs. Among products in development are:
* Giredestrant: Roche
* Amcenestrant (SAR439859): Sanofi
* AZD9833: AstraZeneca
* Rintodestrant: G1 Therapeutics
G1 Therapeutics, Inc. is an American biopharmaceutical company headquartered in Research Triangle Park, North Carolina. The company specializes in developing and commercializing small molecule therapeutics for the treatment of patients with cance ...
* LSZ102: Novartis
* LY3484356: Eli Lilly
* Elacestrant: Radius Health
* ZN-c5: Zentalis
* D-0502 D- means:
* Placed before a U.S. state, usually in parentheses, indicates the person it applies to is a Democratic Party politician of that state. "R-" is used for the Republican Party.
* An academic grade given by certain institutions. Slightly ...
: Inventisbio
* SHR9549: Jiangsu Hengrui Medicine
The oral SERDs target ER-positive/HER2-negative breast cancer and are tested as monotherapy and in combination with other drugs such as the CDK inhibitor palbociclib (Ibrance).
See also
* Aromatase inhibitor
* Estrogen deprivation therapy
Estrogen deprivation therapy, also known as endocrine therapy, is a form of hormone therapy that is used in the treatment of breast cancer. Modalities include antiestrogens or estrogen blockers such as selective estrogen receptor modulators (SERMs) ...
References
Antiestrogens
Hormonal antineoplastic drugs
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