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Toremifene; Anastrozole

Peking Union Medical College Hospital · FDA-approved active Small molecule ✓ Verified May 2026

Toremifene; Anastrozole is a Selective estrogen receptor modulator (SERM) + aromatase inhibitor (AI) Small molecule drug developed by Peking Union Medical College Hospital. It is currently FDA-approved for Hormone receptor-positive breast cancer (metastatic or advanced).

This combination uses toremifene (a selective estrogen receptor modulator) and anastrozole (an aromatase inhibitor) to block estrogen signaling and production in hormone receptor-positive breast cancer.

Toremifene is a small molecule used in the treatment of breast cancer, specifically in postmenopausal women with HER2/Neu negative, invasive, or stage 0 breast cancer. Anastrozole is also used in the treatment of breast cancer, particularly in postmenopausal women, and is often compared to tamoxifen and toremifene in clinical trials.

At a glance

Generic nameToremifene; Anastrozole
SponsorPeking Union Medical College Hospital
Drug classSelective estrogen receptor modulator (SERM) + aromatase inhibitor (AI)
TargetEstrogen receptor (ER); aromatase (CYP19A1)
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved

Mechanism of action

Toremifene acts as a selective estrogen receptor (ER) antagonist in breast tissue, blocking estrogen-driven proliferation of cancer cells. Anastrozole inhibits the aromatase enzyme, reducing peripheral conversion of androgens to estrogen, thereby lowering circulating estrogen levels. Together, they provide dual suppression of estrogen-dependent breast cancer growth through receptor antagonism and hormone depletion.

Approved indications

Common side effects

Key clinical trials

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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Frequently asked questions about Toremifene; Anastrozole

What is Toremifene; Anastrozole?

Toremifene; Anastrozole is a Selective estrogen receptor modulator (SERM) + aromatase inhibitor (AI) drug developed by Peking Union Medical College Hospital, indicated for Hormone receptor-positive breast cancer (metastatic or advanced).

How does Toremifene; Anastrozole work?

This combination uses toremifene (a selective estrogen receptor modulator) and anastrozole (an aromatase inhibitor) to block estrogen signaling and production in hormone receptor-positive breast cancer.

What is Toremifene; Anastrozole used for?

Toremifene; Anastrozole is indicated for Hormone receptor-positive breast cancer (metastatic or advanced).

Who makes Toremifene; Anastrozole?

Toremifene; Anastrozole is developed and marketed by Peking Union Medical College Hospital (see full Peking Union Medical College Hospital pipeline at /company/peking-union-medical-college-hospital).

What drug class is Toremifene; Anastrozole in?

Toremifene; Anastrozole belongs to the Selective estrogen receptor modulator (SERM) + aromatase inhibitor (AI) class. See all Selective estrogen receptor modulator (SERM) + aromatase inhibitor (AI) drugs at /class/selective-estrogen-receptor-modulator-serm-aromatase-inhibitor-ai.

What development phase is Toremifene; Anastrozole in?

Toremifene; Anastrozole is FDA-approved (marketed).

What are the side effects of Toremifene; Anastrozole?

Common side effects of Toremifene; Anastrozole include Hot flashes, Vaginal bleeding/discharge, Arthralgia, Bone loss/osteoporosis, Nausea.

What does Toremifene; Anastrozole target?

Toremifene; Anastrozole targets Estrogen receptor (ER); aromatase (CYP19A1) and is a Selective estrogen receptor modulator (SERM) + aromatase inhibitor (AI).

Related

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing