Elinzanetant
Generic Name: elinzanetant
Brand Names:
Lynkuet
11 DESCRIPTION LYNKUET is an NK1 and NK3 receptor antagonist. The chemical name of elinzanetant is 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]pyridin-3-yl}-N,2-dimethylpropanamide having a molecular formula of C 33 H 35 F 7 N 4 O 3 and a molecular weight of 668.7.
Overview
11 DESCRIPTION LYNKUET is an NK1 and NK3 receptor antagonist. The chemical name of elinzanetant is 2-[3,5-bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]pyridin-3-yl}-N,2-dimethylpropanamide having a molecular formula of C 33 H 35 F 7 N 4 O 3 and a molecular weight of 668.7.
Uses
1 INDICATIONS AND USAGE LYNKUET is indicated for the treatment of moderate to severe vasomotor symptoms (VMS) due to menopause. LYNKUET is a neurokinin 1 (NK1) and neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause. ( 1 )
Dosage
2 DOSAGE AND ADMINISTRATION The recommended dosage is 120 mg (two 60 mg capsules) orally once daily at bedtime with or without food. ( 2.2 ) Swallow capsules whole. Do not cut, crush, or chew capsules. ( 2.2 ) See full prescribing information for LYNKUET dosage modification due to drug interactions. ( 2.3 ) 2.1 Recommended Evaluation and Testing Before Initiation of LYNKUET Exclude pregnancy in females of reproductive potential [see Contraindications (4) ], Warnings and Precautions (5.3) , and Use in Specific Populations (8.3) ].
Side Effects
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Central Nervous System (CNS) Depressant Effect and Daytime Impairment [see Warnings and Precautions (5.1) ] Hepatic Transaminase Elevations [see Warnings and Precautions (5.2) ] The most frequently reported (≥5%) adverse reactions were headache, fatigue, dizziness and somnolence. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bayer HealthCare Pharmaceuticals Inc. at 1-888-842-2937 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Interactions
7 DRUG INTERACTIONS Strong CYP3A4 Inhibitors and grapefruit (juice): Avoid concomitant use with LYNKUET. ( 7.1 ) Moderate CYP3A4 Inhibitors: Reduce LYNKUET dosage to 60 mg once daily. ( 2.2 , 7.1 ) Strong and Moderate CYP3A4 Inducers: Avoid concomitant use with LYNKUET. ( 7.1 ) 7.1 Effects of Other Drugs on LYNKUET Elinzanetant is primarily metabolized via CYP3A4 enzyme. Table 3 describes drug interactions where concomitant use of another drug affects LYNKUET. Table 3: Drug Interactions: Concomitant Use of Other Drugs Affect the Use of LYNKUET Strong and Moderate CYP3A4 Inhibitors See www.fda.gov/CYPandTransporterInteractingDrugs for examples of strong and moderate CYP3A4 inhibitors, and CYP3A4 inducers.
Warnings
5 WARNINGS AND PRECAUTIONS CNS Depressant Effect and Daytime Impairment: Advise patients about the potential for somnolence and other nervous system effects. Advise patients who experience these effects to refrain from driving or engaging in hazardous occupations or activities until the effects have resolved ( 5.1 ) Hepatic Transaminase Elevations: Perform bloodwork prior to initiation of LYNKUET to evaluate for hepatic function and injury. Do not start therapy if serum transaminase concentration is equal to or exceeds two times the upper limit of normal (ULN). Perform follow-up evaluations of hepatic transaminase concentration 3 months after initiation. 4 CONTRAINDICATIONS LYNKUET is contraindicated in pregnancy. Exposure to LYNKUET may cause pregnancy loss or stillbirth when administered during pregnancy [see Use in Specific Populations (8.1 , 8.3) ] . Pregnancy. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary LYNKUET is contraindicated in pregnancy [see Contraindications (4) ]. If pregnancy occurs during the use of LYNKUET, discontinue treatment. Based on findings from animal reproduction studies, LYNKUET may cause pregnancy loss or stillbirth but not fetal malformations when administered during pregnancy. There are no data on the use of LYNKUET in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
Storage
16.2 Storage and Handling Store at 20°C to 25°C (68°F to 77°F) with excursions permitted from 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. For patients requiring a dosage modification (i.e., one 60 mg capsule once daily), instruct them to partially peel back the foil covering of the blister cell exposing only one of the two capsules.
Frequently Asked Questions
What is Elinzanetant used for?▼
1 INDICATIONS AND USAGE LYNKUET is indicated for the treatment of moderate to severe vasomotor symptoms (VMS) due to menopause. LYNKUET is a neurokinin 1 (NK1) and neurokinin 3 (NK3) receptor antagonist indicated for the treatment of moderate to severe vasomotor symptoms due to menopause. ( 1 )
What are the side effects of Elinzanetant?▼
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Central Nervous System (CNS) Depressant Effect and Daytime Impairment [see Warnings and Precautions (5.1) ] Hepatic Transaminase Elevations [see Warnings and Precautions (5.2) ] The most frequently reported (≥5%) adverse reactions were headache, fatigue, dizziness and somnolence. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bayer HealthCare Pharmaceuticals Inc. at 1-888-842-2937 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Can I take Elinzanetant during pregnancy?▼
8.1 Pregnancy Risk Summary LYNKUET is contraindicated in pregnancy [see Contraindications (4) ]. If pregnancy occurs during the use of LYNKUET, discontinue treatment. Based on findings from animal reproduction studies, LYNKUET may cause pregnancy loss or stillbirth but not fetal malformations when administered during pregnancy. There are no data on the use of LYNKUET in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
What are the important warnings for Elinzanetant?▼
5 WARNINGS AND PRECAUTIONS CNS Depressant Effect and Daytime Impairment: Advise patients about the potential for somnolence and other nervous system effects. Advise patients who experience these effects to refrain from driving or engaging in hazardous occupations or activities until the effects have resolved ( 5.1 ) Hepatic Transaminase Elevations: Perform bloodwork prior to initiation of LYNKUET to evaluate for hepatic function and injury. Do not start therapy if serum transaminase concentration is equal to or exceeds two times the upper limit of normal (ULN). Perform follow-up evaluations of hepatic transaminase concentration 3 months after initiation. 4 CONTRAINDICATIONS LYNKUET is contraindicated in pregnancy. Exposure to LYNKUET may cause pregnancy loss or stillbirth when administered during pregnancy [see Use in Specific Populations (8.1 , 8.3) ] . Pregnancy. ( 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.