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tamoxifen + anastrozole + exemestane + letrozole + fulvestrant + toremifene

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

Overview

This entry represents a collection of six distinct pharmaceutical agents—tamoxifen, anastrozole, exemestane, letrozole, fulvestrant, and toremifene—all primarily utilized in the endocrine therapy of hormone receptor-positive breast cancer. These drugs employ varied mechanisms to disrupt estrogen signaling, a key driver of growth in many breast cancers. Tamoxifen and toremifene are Selective Estrogen Receptor Modulators (SERMs), acting as estrogen antagonists in breast tissue while exhibiting partial agonist effects in other tissues like bone and uterus. Anastrozole, exemestane, and letrozole are Aromatase Inhibitors (AIs). Anastrozole and letrozole are non-steroidal and reversibly inhibit the aromatase enzyme, which is responsible for converting androgens into estrogen in postmenopausal women. Exemestane is a steroidal, irreversible aromatase inactivator. Fulvestrant is a Selective Estrogen Receptor Degrader (SERD) and a pure estrogen receptor antagonist, causing the degradation and downregulation of the estrogen receptor protein, thereby completely blocking its activity without any agonist effects. These agents are crucial in both adjuvant and metastatic settings for breast cancer treatment, often used sequentially or in combination with other therapies.

Brand names
NolvadexSoltamoxApo-TamoxCitofenDignotamoxiDuratamoxifen 5Duratamoxifen5Duratamoxifen-5EmblonJenoxifenKessarLedertamNoltamNourytamNovofenOestrifenOncotamRetaximTafoxenTamTamaxinTamifenTamofenTamoneTamoplexTamoxastaTamox-GryTamoxigenatTamox-PurenTaxfenoTerimonValodexZemideZitazoniumArimidexAremedAromasinFemaraKisqali Femara Co-packFaslodexFareston
Other names
TMXICI-46474ICI46474ICI 46474AnastrazoleanastrozolICI-D1033ICI-D-1033ICI-D 1033ZD-1033ZD1033ZD 1033FCE-24304FCE24304FCE 243046-Methylideneandrosta-1,4-diene-3,17-dioneCGS 20267CGS20267CGS-20267ICI-182780ICI182780ICI 182780ZD-182780ZD182780ZD 182780ZD-9238ZD9238ZD 9238(Z)-Toremifene4-Chlorotamoxifen4-CTAcapodeneCCRIS-8745CCRIS8745CCRIS 8745FC-1157FC1157FC 1157FC-1157aFC1157aFC 1157aGTx-006GTx006GTx 006NK-622NK622NK 622NSC-613680NSC613680NSC 613680
02

Targets

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

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