Selective estrogen receptor degrader SERDs)

A selective estrogen receptor degrader or downregulator (SERD) is a type of drug 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-positive or progesterone receptor-positive breast cancer, along with older classes of drugs like selective estrogen receptor modulators (SERMs) and aromatase inhibitors.

Effective for ESR 1 mutations.

SERDs  include fulvestrant, brilanestrant, camizestrant, giredestrant and elacestrant. 

Fulvestrant requires large-volume and frequently painful intramuscular injections.

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 inhibitors.

Elascent is the second SERD to receive approval for ER positive/HER2 negative metastatic breast cancer but its administration is restricted to those with ESR1 mutations.

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