momelotinib dihydrochloride monohydrate: clinical use

Prescribing considerations

• Initiate and monitor under a clinician experienced with anticancer treatment.
• Do not combine with another JAK inhibitor.
• Do not initiate during an active infection; assess previous or chronic hepatitis B.
• Consider cardiovascular, venous thromboembolism, smoking and malignancy risk factors before starting or continuing treatment.
• Review all medicines and herbal products for CYP and transporter interactions.

Contraindications and cautions

• Hypersensitivity to momelotinib or an excipient
• Pregnancy
• Breastfeeding
• The lactose-containing product should not be used in specified rare hereditary disorders of galactose handling.

Monitoring

• Full blood count, including platelets and neutrophils, before treatment and periodically thereafter
• Liver function before treatment and periodically thereafter
• Clinical evidence of infection, bleeding, thrombosis, cardiovascular events and new malignancy
• Hepatitis B activity in patients with chronic infection
• Treatment benefit and tolerability

Clinical pharmacology

Momelotinib and active metabolite M21 inhibit wild-type JAK1/JAK2, mutant JAK2 V617F and ACVR1. Metabolism involves several CYP enzymes, predominantly CYP3A4, followed by aldehyde oxidase pathways; elimination is mainly through metabolism and faecal excretion.

Formulation and product differences

• The selected product is a brown, triangular film-coated tablet marked with an underlined “M” and “150”.
• It contains lactose monohydrate and is essentially sodium-free.
• Store in the original bottle to protect from moisture; leave the desiccant in place and do not swallow it.

Tablet

Route: Oral

Strengths: 100 mg, 150 mg, 200 mg