Drug intelligence / Profile preview

tamoxifen, anastrozole, exemestane, letrozole, fulvestrant, toremifene

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

This entry represents a collective group of six established endocrine therapy agents used as the standard-of-care comparator arm in the CAMERAN Phase 2 clinical trial (sponsored by UNC Lineberger Comprehensive Cancer Center). The group includes selective estrogen receptor modulators (SERMs) like tamoxifen and toremifene, which competitively inhibit estrogen binding to its receptor; aromatase inhibitors (AIs) such as anastrozole, letrozole, and exemestane, which block the peripheral conversion of androgens to estrogens; and the selective estrogen receptor degrader (SERD) fulvestrant, which promotes the downregulation and degradation of the estrogen receptor. These agents are primarily indicated for the treatment of hormone receptor-positive (ER+) breast cancer, particularly in postmenopausal women, by depriving tumor cells of estrogen-mediated growth signals. In the context of the CAMERAN trial, physicians and patients may choose among these six agents as the adjuvant endocrine therapy arm following lumpectomy.

Brand names
NolvadexSoltamoxArimidexAromasinFemaraFaslodexFareston
Other names
Endocrine therapyHormonal therapy
02

Targets

ESR2 (ERβ)ESR1 (ERα)CYP19A1 (Aromatase)

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