Camizestrant
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From MedlinePlus, U.S. National Library of Medicine
Boxed warning
WARNING: ARRHYTHMIA RISK WITH CONCOMITANT USE OF QTc INTERVAL PROLONGING DRUGS ETCAMAH in combination with ribociclib, a QTc interval prolonging drug and a strong CYP3A inhibitor, or in combination with other QTc interval prolonging drugs, can increase the risk of Torsades de Pointes, other ventricular arrhythmias, and sudden death ( 5.1 , 5.2 , 7.1 ). Avoid concomitant use of ETCAMAH with products (other than ribociclib) known to prolong the QTc interval and/or have a known risk of Torsades de Pointes. If concomitant use with other products cannot be avoided, monitor the QTc interval more frequently ( 5.1 , 7.3 ).
Obtain ECG prior to initiation and monitor heart rate and QTc interval during treatment. Assess and correct electrolyte abnormalities prior to initiation and during treatment. Withhold ETCAMAH until resolution of QTc interval prolongation and resume or permanently discontinue ETCAMAH based on severity. ( 2.2 , 2.4 ) WARNING: ARRHYTHMIA RISK WITH CONCOMITANT USE OF QTc INTERVAL PROLONGING DRUGS See full prescribing information for complete boxed warning.
• ETCAMAH in combination with ribociclib, a QTc interval prolonging drug and a strong CYP3A inhibitor, or in combination with other QTc interval prolonging drugs, can increase the risk of Torsades de Pointes, other ventricular arrhythmias, and sudden death ( 5.1 , 5.2 , 7.1 ). • Avoid concomitant use of ETCAMAH with products (other than ribociclib) known to prolong the QTc interval and/or have a known risk of Torsades de Pointes. If concomitant use with other products cannot be avoided, monitor the QTc interval more frequently ( 5.1 , 7.3 ). • Obtain ECG prior to initiation and monitor heart rate and QTc interval during treatment.
Assess and correct electrolyte abnormalities prior to initiation and during treatment. Withhold ETCAMAH until resolution of QTc interval prolongation and resume or permanently discontinue ETCAMAH based on severity ( 2.2 , 2.4 ).
Dosing in kidney impairment
This label has no separate kidney-impairment dosing section. Check warnings and clinical pharmacology in the full label.
Dosing in liver impairment
Dosage in Patients with Hepatic Impairment The recommended dosage for patients with hepatic impairment differs depending on the CDK4/6 inhibitor used in combination with ETCAMAH. For patients with severe (Child-Pugh C) hepatic impairment who are receiving ETCAMAH in combination with ribociclib, the recommended dosage of ETCAMAH is 75 mg once every other day.
For patients with severe (Child-Pugh C) hepatic impairment who are receiving ETCAMAH in combination with abemaciclib or palbociclib, no dosage modification of ETCAMAH is recommended. Monitor patients with moderate (Child-Pugh B) or severe (Child-Pugh C) hepatic impairment receiving ETCAMAH in combination with any CDK4/6 inhibitor for increased adverse reactions and modify the dosage as recommended [see Dosage and Administration].
Preparation and administration
Recommended Dosage and Administration The recommended dosage of ETCAMAH is 75 mg orally once daily, with or without food, until disease progression or unacceptable toxicity [see Clinical Pharmacology] . Administer ETCAMAH in combination with a CDK4/6 inhibitor (abemaciclib, palbociclib, or ribociclib). Continue the CDK4/6 inhibitor at the same dosage as when the ESR1 mutation was detected.
Refer to the Prescribing Information of the CDK4/6 inhibitor for additional dosing information [see Clinical Studies] . Take ETCAMAH at approximately the same time each day. Swallow tablets whole. Do not cut, crush, or chew tablets prior to swallowing. Do not take broken, cracked, or otherwise not intact tablets. If a dose is missed within 6 hours, take the missed dose.
If a dose of ETCAMAH is missed for more than 6 hours, skip the dose for the day and take the next dose at the usual time. If a dose is vomited, do not take an additional dose and take the next dose at the usual time.
Drug interactions
Check camizestrant against a medication listLabel text (11 paragraphs)
7 DRUG INTERACTIONS • CYP3A Inhibitors : Monitor for increased adverse reactions to ETCAMAH with strong CYP3A inhibitors and modify the dosage as recommended. ( 7.1 ) • CYP3A Inducers : Avoid concomitant use of strong and moderate CYP3A inducers. If concomitant use with a moderate CYP3A inducer cannot be avoided, dose adjustment is needed when ETCAMAH is given in combination with abemaciclib or palbociclib.
( 2.6 , 7.1 ) • CYP2C9 and/or CYP2C19 Substrates : Avoid concomitant use of ETCAMAH with CYP2C9 substrates or CYP2C19 substrates during treatment with ETCAMAH and at least 2 weeks after the last dose of ETCAMAH, unless otherwise recommended in the Prescribing Information of the CYP2C9 substrate or CYP2C19 substrate. ( 7.2 ) • CYP3A Substrates : Refer to the Prescribing Information for CYP3A substrates where minimal increases in the concentration may lead to serious adverse reactions. ( 7.2 )
7.1 Effect of Other Drugs on ETCAMAH Table 5 describes drug interactions where concomitant use of another drug affects ETCAMAH. Table 5. Drug Interactions involving ETCAMAH and Other Drug Products Strong CYP3A Inhibitors Prevention or Management • Monitor for increased adverse reactions to ETCAMAH and modify the dosage as recommended [see Dosage and Administration ( 2.4 )]. Mechanism and Clinical Effect • Camizestrant is a CYP3A substrate. Concomitant use with strong CYP3A inhibitors increases camizestrant plasma concentrations [see Clinical Pharmacology ( 12.3 )] , which may increase the risk of adverse reactions related to ETCAMAH.
• ETCAMAH is indicated to be used in combination with CDK4/6 inhibitors, including ribociclib, which is a strong CYP3A inhibitor and can prolong the QT interval [see Warnings and Precautions ( 5.1 ) and Drug Interactions ( 7.3 )] . Strong and Moderate CYP3A Inducers Prevention or Management • Avoid concomitant use of strong CYP3A inducers. • The co-administration of ETCAMAH and a moderate CYP3A inducer is allowed with caution. • The dosage recommendations for concomitant use of moderate CYP3A inducers differ depending on the CDK4/6 inhibitor used in combination with ETCAMAH.
o Avoid concomitant use of moderate CYP3A inducers for patients who are receiving ETCAMAH in combination with abemaciclib or palbociclib. If concomitant use cannot be avoided, increase the ETCAMAH dosage from 75 mg once daily to 150 mg once daily for patients who are receiving ETCAMAH in combination with abemaciclib or palbociclib [see Dosage and Administration ( 2.6 )] . After the moderate CYP3A inducer has been discontinued for at least 14 days, resume the ETCAMAH dosage used prior to initiation of the moderate CYP3A inducer. o For patients who are receiving ETCAMAH in combination with ribociclib concomitantly with a moderate CYP3A inducer, no ETCAMAH dosage modification is recommended.
Mechanism and Clinical Effect • Camizestrant is a CYP3A substrate. Concomitant use with strong or moderate CYP3A inducers decreases camizestrant plasma concentrations [see Clinical Pharmacology ( 12.3 )] which may reduce ETCAMAH effectiveness.
7.2 Effect of ETCAMAH on Other Drugs Table 6 describes drug interactions where concomitant use of ETCAMAH affects another drug. Table 6. Drug Interactions involving ETCAMAH and Other Drug Products CYP2C9 Substrates or CYP2C19 Substrates Prevention or Management • Avoid concomitant use of ETCAMAH with CYP2C9 substrates or CYP2C19 substrates during treatment with ETCAMAH and at least 2 weeks after the last dose of ETCAMAH, unless otherwise recommended in the Prescribing Information of the CYP2C9 substrate or CYP2C19 substrate. Mechanism and Clinical Effect • ETCAMAH is a strong CYP2C9 inhibitor and a strong CYP2C19 inhibitor.
• ETCAMAH is predicted to increase the exposure of both CYP2C9 substrates and CYP2C19 substrates [see Clinical Pharmacology ( 12.3 )] , which may increase the risk of adverse reactions related to these substrates. Certain CYP3A Substrates Prevention or Management • Refer to the Prescribing Information for CYP3A substrates where minimal increases in the concentration may lead to serious adverse reactions. Mechanism and Clinical Effect • ETCAMAH is a CYP3A inhibitor. • ETCAMAH increases exposure of CYP3A substrates [see Clinical Pharmacology ( 12.3 )] , which may increase the risk of adverse reactions related to these substrates.
7.3 Drugs That Prolong the QTc Interval ETCAMAH is indicated in combination with a CDK4/6 inhibitor and there is increased risk of QTc interval prolongation with ribociclib, a strong CYP3A inhibitor that can prolong the QTc interval [see Drug Interactions ( 7.1 )] . Refer to the ribociclib prescribing information for dosage modifications. Avoid concomitant use of ETCAMAH with products (other than ribociclib) known to prolong the QTc interval and/or have a known risk of Torsades de Pointes. If concomitant use with other products cannot be avoided, monitor the QTc interval more frequently [see Warnings and Precautions ( 5.1 )] .
ETCAMAH in combination with a CDK4/6 inhibitor is associated with QTc interval prolongation [see Clinical Pharmacology ( 12.2 )].
7.4 Drugs That Cause Bradycardia Avoid concomitant use of ETCAMAH with other products known to cause bradycardia. Monitor for signs and symptoms of bradycardia if concomitant use cannot be avoided [see Warnings and Precautions ( 5.2 )] . ETCAMAH causes decreases in heart rate that are dose and baseline heart rate dependent [see Clinical Pharmacology ( 12.2 )] .
Contraindications
None. None. (4)
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
LiverTox has no chapter for camizestrant. Check the label's hepatic warnings.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action, ETCAMAH can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available human data on ETCAMAH use in pregnant women to inform the drug-associated risk. In animal reproduction studies, oral administration of camizestrant to rats during pregnancy resulted in adverse developmental outcomes including embryo-fetal/neonatal mortality and alterations to growth at maternal exposures below the human AUC at the recommended dose (see Data) . Advise pregnant women and females of reproductive potential of the potential risk to a fetus. In the U.S.
general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2%-4% and 15%-20%, respectively. Data Animal Data In an embryo-fetal development study with pre- and post-natal assessments, female rats received camizestrant at doses of 0.1 mg/kg from gestation Day (GD) 2 to 20, doses up to 0.091 mg/kg from GD 6 to 16, or doses of 0.075 and 0.75 mg/kg from GD 6 to lactation day (LD) 6. Administration of 0.1 mg/kg camizestrant during GD 2 to 20 resulted in no pregnancies.
Camizestrant at doses ≥ 0.075 mg/kg administered from GD 6 to LD 6 resulted in increased length of gestation, dystocia, and decreased pup survival and pup weight. At all doses, maternal exposures were below the human AUC at the recommended dose.
For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.
Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
Price ladder
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