Capivasertib

Capivasertib is a prescription medication indicated in combination with fulvestrant for hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer with 1 and more PIK3CA/AKT1/PTEN-alterations, following progression on at least 1 endocrine-based regimen in the metastatic setting or recurrence on or within 12 months of completing adjuvant therapy

• Capivasertib is available under the following different brand names: Truqap.

Common side effects of Capivasertib include:

• diarrhea
• increased random glucose 
• cutaneous adverse reaction 
• decreased lymphocytes
• decreased hemoglobin 
• fatigue 
• increased fasting glucose 
• nausea 
• decreased leukocytes 
• increased triglycerides 
• stomatitis
• decreased neutrophils 
• vomiting

Serious side effects of Capivasertib include:

• cutaneous adverse reaction
• diarrhea
• pneumonia
• vomiting
• pyrexia
• hyperglycemia
• hypersensitivity
• fatigue
• renal injury
• second malignancy
• sepsis
• acute myocardial infarction

Rare side effects of Capivasertib 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

Tablet

• 160 mg
• 200 mg

Breast Cancer

Adult dosage

• Capivasertib weekly dose schedule
  • 400 mg orally twice daily (~12 hours apart) for 4 consecutive days followed by 3 days off
  • Repeat weekly schedule until disease progression or unacceptable toxicity
• Fulvestrant regimen during clinical trial
• 28-day cycles
  • Cycle 1: 500 mg IM cycle 1 on day 1 and 15
  • Subsequent cycles: 500 mg IM on day 1
• Premenopausal and perimenopausal women: Administer a luteinizing hormone-releasing hormone (LHRH) agonist according to current clinical practice standards
• Men: Consider administering a LHRH agonist according to current clinical practice standards

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.

• Capivasertib has severe interactions with no other drugs
• Capivasertib has serious interactions with at least 69 other drugs
• Capivasertib has moderate interactions with at least 43 other drugs
• Capivasertib has minor interactions with the following drug:
  • diltiazem

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

• Severe hypersensitivity to capivasertib or any of its components

Effects of drug abuse

• None

Short-Term Effects

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

Long-Term Effects

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

Cautions

• May cause fetal harm, based on findings from animals and mechanism of action
• Hyperglycemia
  • Severe hyperglycemia associated with ketoacidosis occurred in clinical trials
  • Safety has not been established in patients with type I diabetes or diabetes requiring insulin; patients with insulin-dependent diabetes were excluded from clinical trials
  • Evaluate fasting glucose (FG) before initiating and during treatment
  • If hyperglycemia occurs after treatment, monitor FG as clinically indicated, and at least twice weekly until FG decreases to normal levels
  • See dosage modifications if the patient experiences hyperglycemia during treatment
• Diarrhea
  • Severe diarrhea associated with dehydration may occur
  • Monitor for signs and symptoms of diarrhea
  • Advise patients to increase oral fluids and start antidiarrheal treatment at the first sign of diarrhea while taking capivasertib
• Cutaneous reactions
  • Cutaneous adverse reactions may occur, which can be severe, including erythema multiforme, palmoplantar erythrodysesthesia, and drug reaction with eosinophilia and systemic symptoms
  • Monitor for signs and symptoms of cutaneous reactions
• Drug interaction overview
• CYP3A substrate
  • Strong CYP3A inhibitors
    • Avoid coadministration; if unable to avoid reduce capivasertib dose and monitor for adverse effects
    • Strong CYP3A inhibitors increase capivasertib exposure
  • Moderate CYP3A inhibitors
    • Modify dose
    • Moderate CYP3A inhibitors increase capivasertib exposure; reduce capivasertib dose if coadministered
  • Strong or moderate CYP3A inducers
    • Avoid coadministration
    • Strong or moderate CYP3A inducers decrease capivasertib exposure, which may reduce efficacy

Pregnancy and Lactation

• Based on findings in animals and mechanism of action, can cause fetal harm when administered to pregnant women
• Advise pregnant women and those who are of reproductive potential of potential fetal risk
• Verify the pregnancy status of females of reproductive potential before initiating
• Contraception
  • Females of reproductive potential: Use effective contraception during treatment with and for 1 month after the last dose
  • Males with female partners of reproductive potential: Use effective contraception during treatment with and for 4 months after the last dose
• Lactation
  • Data are unavailable regarding the presence of capivasertib or its metabolites in human milk or their effects on milk production or breastfed children
  • Advise women not to breastfeed during treatment