Asciminib

Asciminib is a prescription medication indicated for Philadelphia chromosome–positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP) in adults previously treated with ≥2 tyrosine kinase inhibitors (TKIs).

• Asciminib is available under the following different brand names: Scemblix

Common side effects of Asciminib include:

• upper respiratory tract infections
• musculoskeletal pain
• fatigue
• nausea
• rash
• diarrhea
• decreased platelet count
• increased level of triglycerides
• decreased neutrophil count
• decreased hemoglobin level
• increased creatine kinase
• increased alanine aminotransferase
• increased lipase
• increased amylase

Serious side effects of Asciminib include:

• hives
• difficulty breathing
• swelling of the face, lips, tongue, or throat
• severe dizziness
• unusual bleeding
• easy bruising
• any bleeding
• blood in the urine
• black or tarry stools
• fever
• persistent sore throat
• pancreatitis
• stomach pain
• nausea
• vomiting
• confusion
• headache
• chest pain
• shortness of breath
• skin rash
• flushing
• fast or abnormal heartbeat
• heart attack
• stroke
• blood clots or blockage
• heart failure
• swelling in the ankles or feet
• weight gain
• numbness or weakness on one side of their body
• decreased vision
• loss of vision
• trouble talking
• pain in the arms, legs, back, neck, or jaw
• severe stomach pain

Rare side effects of Asciminib include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablets

• 20 mg
• 40 mg

Chronic myeloid leukemia

Adult dosage

• Previously treated patients
  • 80 mg orally once a day OR 40 mg orally every 12 hours
  • Continue until disease progression or unacceptable toxicity occurs
• Patients with T315I mutation
  • 200 mg orally every 12 hours
  • Continue until disease progression or unacceptable toxicity occurs

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Asciminib has severe interactions with no other drugs.
• Asciminib has serious interactions with no other drugs.
• Asciminib has moderate interactions with the following drug:
  • warfarin
• Asciminib has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Asciminib?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Asciminib?”

Cautions

• Thrombocytopenia, neutropenia, and anemia occurred; perform complete blood cell counts every 2 weeks for the first 3 months of treatment and monthly thereafter or as clinically indicated; monitor for signs and symptoms of myelosuppression; advise patients to immediately report fever, any suggestion of infection, or signs or symptoms suggestive of bleeding or easy bruising
• Hypertension reported; monitor and manage hypertension using standard antihypertensive therapy during treatment as clinically indicated; advise patients to contact a healthcare provider for elevated blood pressure or if symptoms of hypertension occur including confusion, headache, dizziness, chest pain, or shortness of breath
• Hypersensitivity reactions (eg, rash, edema, bronchospasm) reported; monitor for signs and symptoms of hypersensitivity and initiate appropriate treatment as clinically indicated
• Based on findings from animal studies and its mechanism of action, fetal harm may occur when administered to pregnant women
• Pancreatitis
  • Pancreatitis reported
  • Assess serum lipase and amylase levels monthly during treatment or as clinically indicated; monitor for signs and symptoms of pancreatic toxicity
  • Perform more frequent monitoring in patients with a history of pancreatitis
  • If lipase and amylase elevation are accompanied by abdominal symptoms, temporarily withhold therapy, and consider appropriate diagnostic tests to exclude pancreatitis
  • Inform patients to report to healthcare professionals symptoms of pancreatitis, including nausea, vomiting, severe abdominal pain, or abdominal discomfort
• Cardiovascular toxicity
  • Cardiovascular toxicity (including ischemic cardiac and CNS conditions, arterial thrombotic and embolic conditions) and cardiac failure reported
  • Cardiovascular toxicity reported in patients with preexisting cardiovascular conditions or risk factors, and/or prior exposure to multiple TKIs
  • Arrhythmia, including QTc prolongation, reported
  • Monitor patients with a history of cardiovascular risk factors for cardiovascular signs and symptoms; initiate appropriate treatment as clinically indicated
  • Cardiac electrophysiology testing showed Asciminib does not cause a large mean increase in QTc interval (i.e., above 20 msec) at the maximum dose (200 mg two times a day); based on available clinical data, a small mean QTc increase (below 10 msec) cannot be excluded
• Drug interaction overview
  • CYP3A4 substrate
    • Inhibitor of CYP3A4, CYP2C9, and P-glycoprotein (P-gp)
  • Strong CYP3A4 inhibitors
    • Closely monitor for adverse reactions, especially in patients treated at 200 mg every 12 hours
    • Strong CYP3A4 inhibitor increases both plasma concentrations and the risk for toxicities of asciminib
    • Itraconazole oral solution containing hydroxypropyl-β-cyclodextrin
    • Avoid coadministration
    • Itraconazole oral solution containing hydroxypropyl-β-cyclodextrin decreases asciminib plasma concentration and efficacy
  • Sensitive CYP3A4 substrates
    • 80 mg/day dosing: Closely monitor for adverse reactions
    • 200 mg every 12 hours dosing: Avoid coadministration
    • Asciminib increases plasma levels of sensitive CYP3A4 substrates and the risk for adverse reactions of these substrates
• Sensitive CYP2C9 substrates
  • Avoid coadministration
  • 80 mg/day-dosing: If coadministration is unavoidable, consider reducing CYP2C9 substrate dosage as recommended in its prescribing information
  • 200 mg every 12-hour-dosing: If coadministration is unavoidable, consider alternative therapy with a non-CYP2C9 substrate
  • Asciminib increases plasma levels and the risk for adverse reactions of sensitive CYP2C9 substrates
• Sensitive P-gp substrates
  • Closely monitor for adverse reactions of P-gp substrates
  • Asciminib increases the plasma concentrations of P-gp substrates and the risk for adverse reactions

Pregnancy and Lactation

• Based on animal studies and the drug’s mechanism of action, embryofetal harm may occur when administered to pregnant women
• There are no available data on the use of asciminib in pregnant women to evaluate any drug-associated risks
• Verify the pregnancy status of women of reproductive potential before initiating therapy
• Contraception
  • Females of reproductive potential: Use effective contraception during treatment and for 1 week after the last dose
• Infertility
  • Based on animal studies, fertility may be impaired in women of reproductive potential; the reversibility of the effect on fertility is unknown
• Lactation
  • There are no data on the presence of asciminib or its metabolites in human milk, its effects on breastfed infants, or its effects on milk production
  • Advise women not to breastfeed during the treatment and for 1 week after the last dose