Abemaciclib

Cytostatic · Kinase inhibitors

Indications

: (1) In combination with endocrine therapy (tamoxifen or an aromatase inhibitor) for the adjuvant treatment of adult pts with HR+ve, HER2-ve, node+ve, early breast cancer at high risk of recurrence and a Ki-67 score =20%. (2) In combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women, and men with HR+ve, HER2-ve advanced or metastatic breast cancer. (3) In combination with fulvestrant for the treatment of adult pts with HR+ve, HER2-ve advanced or metastatic breast cancer with disease progression following endocrine therapy. (4) As monotherapy for the treatment of adult pts with HR+ve, HER2-ve advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting.

Dosage

Adults: In combination with fulvestrant, tamoxifen, or an aromatase inhibitor: Initially 150 mg twice daily. As monotherapy: 200 mg twice daily. Children: Not recommended.

Adverse Effects

Nausea, vomiting, headache, diarrhoea, abdominal pain, neutropaenia, leucopaenia, thrombocytopaenia, fatigue, infections, reduced appetite, alopaecia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Grade 3 or 4 ILD or pneumonitis. Precautions: Monitor complete blood counts prior to the start of treatment, every 2 wks for the first 2 months, monthly for the next 2 months, and as clinically indicated. Monitor for clinical symptoms or radiological changes indicative of ILD/pneumonitis. Severe hepatic impairment; perform LFTs before starting treatment, every 2 wks for the first 2 months, monthly for the next 2 months, and as clinically indicated. Monitor for signs and symptoms of thrombosis and pulmonary embolism.

Interactions

CYP3A inhibitors e.g. ketoconazole, clarithromycin, verapamil and diltiazem. CYP3A inducers e.g. rifampin, efavirenz, bosentan, modafinil. Loperamide. Metformin.

Advice to Patient

Take with or without meals. Swallow whole tabs. Do not chew, crush or split tabs before swallowing. Do not ingest tab if broken, cracked or otherwise not intact. Take dose at the same time every day. If vomit occurs or a dose is missed, take the next dose at its scheduled time. Start antidiarrhoeal therapy such as loperamide at the first sign of loose stools, increase oral fluids, and report physician for further instructions and follow up. Females of reproductive potential must use effective contraception during treatment and for 3 wks after the last dose. Lactating females must avoid nursing babies during treatment and for 3 wks after the last dose. Report fever, signs of infection, new or worsening respiratory symptoms, pain or swelling in an extremity, shortness of breath, chest pain, tachypnoea, and tachycardia.

Pharmacokinetics

Bioavailability: Absolute: 200 mg dose: 45%. Metabolism: Hepatic. Half-life elimination: 18.3 hrs. Time to peak: 8 hrs. Excretion: Faeces (81%). Urine (3%).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.