abemaciclib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
abemaciclib: clinical details
Prescribing considerations
- Initiation and supervision should be by clinicians experienced in anticancer treatment.
- Act promptly on diarrhoea with antidiarrhoeal treatment, oral fluids and toxicity assessment.
- Assess new respiratory symptoms for interstitial lung disease or pneumonitis.
- Consider venous and arterial thromboembolic risk and symptoms.
- Use caution in severe renal impairment because evidence is limited; severe hepatic impairment increases exposure.
- Review CYP3A4 inhibitors, inducers and transporter substrates before prescribing.
Contraindications and cautions
- Hypersensitivity to abemaciclib or any excipient.
- The tablets contain lactose and should not be used in rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.
Monitoring
- Check full blood count and ALT and AST before treatment, frequently during early treatment and subsequently as clinically indicated.
- Monitor bowel symptoms, hydration, infection, pulmonary symptoms and venous or arterial thromboembolism.
- An isolated creatinine rise may reflect inhibited tubular secretion rather than reduced glomerular function; use alternative renal markers when clinically appropriate.
Clinical pharmacology
Abemaciclib and active metabolites inhibit CDK4 and CDK6. It is mainly metabolised hepatically by CYP3A4 and inhibits several renal and efflux transporters, including OCT2, MATE1, MATE2-K, P-gp and BCRP.
Formulation and product differences
- Available as oral film-coated tablets in several strengths; colour and size differ by strength.
- All selected tablets contain lactose, are essentially sodium-free and must be swallowed whole.
abemaciclib interactions
The cancer team and pharmacist should review prescribed, over-the-counter and herbal products before and during treatment.
Strong CYP3A4 inhibitors, including clarithromycin, itraconazole, ketoconazole, posaconazole, voriconazole and lopinavir/ritonavir
These can substantially increase abemaciclib exposure and toxicity, so concurrent use should generally be avoided or specialist-managed.
Strong CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin and St John’s wort
These can markedly reduce abemaciclib exposure and potentially reduce its effectiveness, so concurrent use should be avoided.
Grapefruit and grapefruit juice
These may increase abemaciclib concentrations and should be avoided.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.