Imlunestrant

INLURIYO is indicated: as monotherapy, for the treatment of adults with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 (ESR1 )-mutated advanced or metastatic breast cancer, as detected by an FDA-authorized test, with disease progression following at least one line of endocrine therapy. in combination with abemaciclib for the treatment of adults with ER-positive, HER2-negative, ESR1 -mutated advanced or metastatic breast cancer, as detected by an FDA-authorized test, with disease progression following at least one line of endocrine therapy.

Imlunestrant is an estrogen receptor (ER) antagonist that binds to ERα. In vitro, imlunestrant induced degradation of ERα, leading to inhibition of ER-dependent gene transcription and cellular proliferation in ER+ breast cancer cells. Imlunestrant demonstrated in vitro and in vivo anti-tumor activity in ER+ breast cancer xenograft models, including models with ESR1 mutations.

Select patients for treatment based on the presence of ESR1 mutations. The recommended dosage is 400 mg orally once daily, on an empty stomach at least 2 hours before food or 1 hour after food. See Full Prescribing Information for dosage modifications. For patients with moderate or severe hepatic impairment, the recommended dosage is 200 mg orally once daily.

None. None.

Embryo-Fetal Toxicity: INLURIYO can cause fetal harm. Advise of the potential risk to a fetus and to use effective contraception. Embryo-Fetal Toxicity Based on findings in animals and its mechanism of action, INLURIYO can cause fetal harm when administered to a pregnant woman. In an animal reproduction study, oral administration of imlunestrant to pregnant rats during the period of organogenesis led to embryo-fetal mortality and structural abnormalities at maternal exposures that were below the human exposure at the recommended dose based on AUC. Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with INLURIYO and for 1 week after the last dose.

The most common (incidence ≥10%) adverse reactions, including laboratory abnormalities, for INLURIYO monotherapy were: decreased hemoglobin, musculoskeletal pain, decreased calcium, decreased neutrophils, increased AST, fatigue, diarrhea, increased ALT, increased triglycerides, nausea, decreased platelets, constipation, increased cholesterol, and abdominal pain. The most common (incidence ≥ 10%) adverse reactions, including laboratory abnormalities, for INLURIYO in combination with abemaciclib were decreased neutrophils, diarrhea, decreased hemoglobin, decreased lymphocytes, nausea, decreased platelets, fatigue, increased triglycerides, infections, increased AST, increased creatinine, increased ALT, vomiting, musculoskeletal pain, abdominal pain, decreased appetite, increased cholesterol, rash, cough, headache, and decreased weight.

Strong CYP3A Inhibitors: Avoid concomitant use with INLURIYO. If concomitant use cannot be avoided, decrease the INLURIYO dosage. Strong CYP3A Inducers: Avoid concomitant use with INLURIYO. If concomitant use cannot be avoided, increase the INLURIYO dosage.

Store at 20°C to 25°C (68°F to 77°F). Excursions between 15°C to 30°C (59°F to 86°F) are permitted.