Imlunestrant
Generic Name: imlunestrant
Brand Names:
Inluriyo
11 DESCRIPTION INLURIYO tablets contain imlunestrant, an estrogen receptor antagonist. The chemical name for imlunestrant tosylate is (5R)-5-(4-(2-(3-(flouromethyl)azetidin-1-yl)ethoxy)phenyl)-8-(trifluoromethyl)-5H-( 1 )benzopyrano(4,3-c)quinolin-2-ol, tosylate salt (1:1). Imlunestrant tosylate is a white to practically white to yellow powder with the empirical formula C 29 H 24 F 4 N 2 O 3 .C 7 H 8 O 3 S and a molecular weight 696.71 g/mol.
Overview
11 DESCRIPTION INLURIYO tablets contain imlunestrant, an estrogen receptor antagonist. The chemical name for imlunestrant tosylate is (5R)-5-(4-(2-(3-(flouromethyl)azetidin-1-yl)ethoxy)phenyl)-8-(trifluoromethyl)-5H-( 1 )benzopyrano(4,3-c)quinolin-2-ol, tosylate salt (1:1). Imlunestrant tosylate is a white to practically white to yellow powder with the empirical formula C 29 H 24 F 4 N 2 O 3 .C 7 H 8 O 3 S and a molecular weight 696.71 g/mol.
Uses
1 INDICATIONS AND USAGE INLURIYO is indicated 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 with disease progression following at least one line of endocrine therapy. INLURIYO TM is an estrogen receptor antagonist indicated for: treatment of adults with ER-positive, HER2-negative, ESR1 -mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy ( 1 )
Dosage
2 DOSAGE AND ADMINISTRATION Select patients for treatment based on the presence of ESR1 mutations. ( 2.1 ) The recommended dosage is 400 mg orally once daily, on an empty stomach. ( 2.2 ) Reduce the dose in patients with moderate or severe hepatic impairment ( 2.4 , 8.6 ) Dosage modifications may be required. ( 2.3 , 2.4 , 2.5 ) 2.1 Patient Selection Select patients for treatment of ER-positive, HER2-negative advanced or metastatic breast cancer with INLURIYO based on the presence of ESR1 mutation(s) in a plasma specimen using an FDA-approved test [see Indications and Usage ( 1 ) and Clinical Studies (14.1)] . Information on FDA-approved tests for the detection of ESR1 mutations in breast cancer is available at: https://www.fda.gov/CompanionDiagnostics .
Side Effects
6 ADVERSE REACTIONS The most common (incidence ≥10%) adverse reactions, including laboratory abnormalities were: hemoglobin decreased, musculoskeletal pain, calcium decreased, neutrophils decreased, AST increased, fatigue, diarrhea, ALT increased, triglycerides increased, nausea, platelets decreased, constipation, cholesterol increased, and abdominal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Eli Lilly and Company at 1-800-LillyRx (1-800-545-5979) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Interactions
7 DRUG INTERACTIONS Strong CYP3A Inhibitors: Avoid concomitant use with INLURIYO. If concomitant use cannot be avoided, decrease the INLURIYO dosage. ( 2.5 , 7.1 ) Strong CYP3A Inducers: Avoid concomitant use with INLURIYO. If concomitant use cannot be avoided, increase the INLURIYO dosage ( 2.5 , 7.1 ). 7.1 Effects of Other Drugs on INLURIYO Strong CYP3A Inhibitors Avoid concomitant use of INLURIYO with strong CYP3A inhibitors. If concomitant use cannot be avoided, reduce the dosage of INLURIYO [see Dosage and Administration ( 2.5 ), Clinical Pharmacology ( 12.3 )] . Imlunestrant is a CYP3A substrate. Concomitant use of a strong CYP3A inhibitor increases imlunestrant exposure [see Clinical Pharmacology ( 12.3 )] , which may increase the risk of INLURIYO-associated adverse reactions.
Warnings
5 WARNINGS AND PRECAUTIONS Embryo-Fetal Toxicity: INLURIYO can cause fetal harm. Advise of the potential risk to a fetus and to use effective contraception. ( 5.1 , 8.1 , 8.3 ) 5.1 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. 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action, INLURIYO can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available human data on INLURIYO use in pregnant women to inform the drug-associated risk. 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 below the human exposure at the recommended dose based on AUC ( see Data ).
Storage
Storage and Handling 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 [see USP Controlled Room Temperature] .
Frequently Asked Questions
What is Imlunestrant used for?▼
1 INDICATIONS AND USAGE INLURIYO is indicated 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 with disease progression following at least one line of endocrine therapy. INLURIYO TM is an estrogen receptor antagonist indicated for: treatment of adults with ER-positive, HER2-negative, ESR1 -mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy ( 1 )
What are the side effects of Imlunestrant?▼
6 ADVERSE REACTIONS The most common (incidence ≥10%) adverse reactions, including laboratory abnormalities were: hemoglobin decreased, musculoskeletal pain, calcium decreased, neutrophils decreased, AST increased, fatigue, diarrhea, ALT increased, triglycerides increased, nausea, platelets decreased, constipation, cholesterol increased, and abdominal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Eli Lilly and Company at 1-800-LillyRx (1-800-545-5979) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Can I take Imlunestrant during pregnancy?▼
8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action, INLURIYO can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available human data on INLURIYO use in pregnant women to inform the drug-associated risk. 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 below the human exposure at the recommended dose based on AUC ( see Data ).
What are the important warnings for Imlunestrant?▼
5 WARNINGS AND PRECAUTIONS Embryo-Fetal Toxicity: INLURIYO can cause fetal harm. Advise of the potential risk to a fetus and to use effective contraception. ( 5.1 , 8.1 , 8.3 ) 5.1 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. 4 CONTRAINDICATIONS None. None. ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.