Capivasertib, a kinase inhibitor, is an antineoplastic agent.1
Capivasertib is used in combination with fulvestrant for the treatment of adults with hormone receptor (HR)-positive, human epidermal growth factor receptor type 2 (HER2)-negative, locally advanced or metastatic breast cancer with 1 or more PIK3CA/AKT1/PTEN -alterations as detected by an FDA-approved test following progression on ≥1 endocrine-based regimen in the metastatic setting or recurrence on or within 12 months of completing adjuvant therapy.1
The current indication for capivasertib is based principally on the results of randomized, double-blind, multicenter clinical trial (CAPItello-291).1, 2 Eligible patients were adults with HR-positive, HER2-negative locally advanced (inoperable) or metastatic breast cancer.1, 2 All patients were required to have progression on an aromatase inhibitor (with or without a CDK4/6 inhibitor) in the metastatic setting, or recurrence on or within 12 months of completing neoadjuvant/adjuvant treatment with an aromatase inhibitor.1, 2 Patients were allowed to have received ≤2 prior lines of endocrine therapy and ≤1 line of chemotherapy for locally advanced or metastatic disease.1, 2 Enrolled patients were randomized 1:1 to receive either capivasertib (400 mg orally twice daily for 4 days, followed by 3 days off treatment each week of the 28-day treatment cycle) plus fulvestrant (500 mg intramuscularly every 14 days for the first 3 injections and every 28 days thereafter) or matching placebo plus fulvestrant.1, 2 Treatment was continued until disease progression or unacceptable toxicity occurred.1, 2 The primary efficacy endpoints were investigator-assessed progression-free survival in the overall population and in the population of patients with AKT pathway-altered ( PIK3CA , AKT1 , or PTEN ) tumors.1, 2 Additional efficacy endpoints included overall survival, investigator-assessed objective response rate, and duration of response.1
A total of 708 patients underwent randomization in the CAPItello-291 trial, of which 289 patients had tumors with AKT pathway alterations.1 The median patient age was 59 years; 99% of patients were female, 52% were white, 29% were Asian, and 9% were Hispanic/Latino.1 The Eastern Cooperative Oncology Group (ECOG) performance status was 0 or 1 in 66 or 34% of patients, respectively.1 Eighteen percent of patients were premenopausal or perimenopausal; 76, 13, and 17% of patients had an alteration in PIK3CA, AKT1, and PTEN, respectively.1 All patients received prior endocrine-based therapy, including an aromatase inhibitor; 71% of patients received prior CDK4/6 inhibitor therapy, and 18% received prior chemotherapy for locally advanced or metastatic disease.1
At the time of the primary analysis, the median duration of treatment with capivasertib or placebo was 5.4 or 3.6 months, respectively, with a median duration of treatment with fulvestrant of 5.8 months in the capivasertib group and 3.7 months in the placebo group.2 In the overall population, the median progression-free survival was 7.2 months in the capivasertib-fulvestrant group and 3.6 months in the placebo-fulvestrant group.2 In the AKT pathway-altered population, there were 121 and 115 events of progression or death in the capivasertib-fulvestrant and placebo-fulvestrant groups, respectively, with a median progression-free survival of 7.3 months and 3.1 months, respectively.1, 2 Overall survival results were not mature at the time of primary analysis of progression-free survival; 30% of the patients died.1 The objective response rate was 26% in the capivasertib-fulvestrant group and 8% in the placebo-fulvestrant group.1 The median duration of response was 10.2 and 8.6 months in the capivasertib-fulvestrant and placebo-fulvestrant groups, respectively.1
Guidelines from the American Society of Clinical Oncology (ASCO) provide recommendations for the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer.3 The guideline supports the use of capivasertib in combination with fulvestrant as a treatment option.3 ASCO recommends CDK4/6 inhibitor therapy with endocrine therapy as first-line treatment.3 Second and third-line treatment options include targeted therapies (e.g., capivasertib, alpelisib) based on tumor genomics and prior endocrine therapy.3 For tumors harboring PIK3CA or AKT1 mutations or PTEN inactivation, capivasertib in combination with endocrine therapy is appropriate.3 Alpelisib combined with endocrine therapy is also an option for tumors harboring PIK3CA mutations, but not AKT1 mutations or PTEN inactivation.3 No comparative efficacy data are available to guide selection between capivasertib or alpelisib when targeting PIK3CA mutations; therefore, ASCO recommends choosing the targeted agent based on perceived risk-benefit considerations (e.g., hyperglycemia, diarrhea, or treatment discontinuation for adverse events).3
Capivasertib is available as tablets containing 160 mg or 200 mg of the drug.1
Administer the tablets orally with or without food.1 Swallow tablets whole; do not split, crush, or chew prior to swallowing.1 Do not take tablets that are broken, cracked, or otherwise not intact.1
If a dose of capivasertib is missed within 4 hours of the scheduled time, take the missed dose.1 If more than 4 hours has passed, skip the missed dose and take the next dose at the regularly scheduled time.1
If a dose of capivasertib is vomited, do not to take an extra dose; take next dose at the regularly scheduled time.1
Store capivasertib tablets in the original bottle at 20-25ºC (excursions permitted between 15-30ºC).1
For use in combination with fulvestrant for the treatment of HR-positive, HER2-negative, PIK3CA/AKT1/PTEN -mutated, advanced or metastatic breast cancer in adults with disease progression following endocrine therapy, the recommended dosage of capivasertib is 400 mg (two 200-mg tablets) administered orally twice daily (approximately 12 hours apart) for 4 days followed by 3 days off.1
Continue treatment until disease progression or unacceptable toxicity occurs.1
Dosage Modification for Toxicity
Temporary interruption of therapy, dosage reduction, and/or permanent discontinuance of capivasertib may be necessary in patients experiencing certain adverse effects.1
If dosage modification is required, reduce the dosage of capivasertib as outlined in Table 1.1 See Table 2 for recommended capivasertib dosage modifications for adverse reactions.1
Dose Reduction | Capivasertib Dose and Schedule |
|---|---|
First dose reduction | 320 mg twice daily for 4 days followed by 3 days off |
Second dose reductiona | 200 mg twice daily for 4 days followed by 3 days off |
aPermanently discontinue capivasertib if unable to tolerate the second dose reduction.1
Adverse Reaction | Severity | Dosage Modification |
|---|---|---|
Hyperglycemia | Fasting glucose (FG) greater than upper limit of normal (ULN) to 160 mg/dL or FG greater than ULN to 8.9 mmol/L or Hemoglobin A1c>7% | Consider initiation or intensification of oral diabetes treatment |
Hyperglycemia | FG 161-250 mg/dL or FG 9-13.9 mmol/L | Withhold capivasertib until FG decrease ≤160 mg/dL (or ≤8.9 mmol/L) If recovery occurs in ≤28 days, resume capivasertib at same dose If recovery occurs in >28 days, resume capivasertib at one lower dose |
Hyperglycemia | FG 251-500 mg/dL or FG 14-27.8 mmol/L | Withhold capivasertib until FG decrease ≤160 mg/dL (or ≤8.9 mmol/L) If recovery occurs in ≤28 days, resume capivasertib at one lower dose If recovery occurs in >28 days, permanently discontinue capivasertib |
Hyperglycemia | FG >500 mg/dL or FG >27.8 mmol/L or Life-threatening sequelae of hyperglycemia at any FG level | Withhold capivasertib For life-threatening sequelae of hyperglycemia or if FG persists at ≥500 mg/dL after 24 hours, permanently discontinue capivasertib If FG ≤500 mg/dL (or ≤27.8 mmol/L) within 24 hours, then follow the guidance in the table for the relevant grade |
Diarrhea | Grade 2 | Withhold capivasertib until recovery to grade 1 or lower If recovery occurs in ≤28 days, resume capivasertib at same dose or one lower dose as clinically indicated If recovery occurs in >28 days, resume at one lower dose as clinically indicated For recurrence, reduce capivasertib by one lower dose |
Diarrhea | Grade 3 | Withhold capivasertib until recovery to grade 1 or lower If recovery occurs in ≤28 days, resume capivasertib at same dose or one lower dose as clinically indicated If recovery occurs in >28 days, permanently discontinue capivasertib |
Diarrhea | Grade 4 | Permanently discontinue capivasertib |
Cutaneous adverse reactions | Grade 2 | Withhold capivasertib until recovery to grade 1 or lower; resume capivasertib at the same dose Persistent or recurrent reactions: reduce capivasertib by one lower dose |
Cutaneous adverse reactions | Grade 3 | Withhold capivasertib until recovery to grade 1 or lower If recovery occurs in ≤28 days, resume capivasertib at same dose If recovery occurs in >28 days, resume at one lower dose For recurrent grade 3 reactions, permanently discontinue capivasertib |
Cutaneous adverse reactions | Grade 4 | Permanently discontinue capivasertib |
Other adverse reactions | Grade 2 | Withhold capivasertib until recovery to grade 1 or lower Resume capivasertib at the same dose |
Other adverse reactions | Grade 3 | Withhold capivasertib until recovery to grade 1 or lower If recovery occurs in ≤28 days, resume capivasertib at same dose If recovery occurs in >28 days, resume at one lower dose |
Other adverse reactions | Grade 4 | Permanently discontinue capivasertib |
Dosage Modification for Concomitant Use with CYP3A4 Inhibitors
When used concomitantly with a moderate CYP3A inhibitor, reduce dosage to 320 mg twice daily for 4 days followed by 3 days off; monitor for adverse reactions.1
Concomitant use with a strong CYP3A inhibitor should be avoided.1 If concomitant use is necessary, reduce dosage of capivasertib to 320 mg orally twice daily for 4 days followed by 3 days off; monitor for adverse reactions.1
After discontinuation of a strong or moderate CYP3A inhibitor, resume the capivasertib dosage (after 3-5 half-lives of the inhibitor) that was taken prior to initiating the strong or moderate CYP3A inhibitor.1
No dosage modification is recommended for patients with mild hepatic impairment (bilirubin less than or equal to upper limit of normal [ULN] and AST greater than ULN, or bilirubin greater than 1-1.5 times ULN and any AST).1
Monitor patients with moderate hepatic impairment (bilirubin greater than 1.5-3 times ULN and any AST) for adverse reactions due to potential increased capivasertib exposure.1
Capivasertib has not been studied in patients with severe hepatic impairment (bilirubin greater than 3 times ULN and any AST).1
No dosage modification is recommended for patients with mild to moderate renal impairment (creatinine clearance [Clcr] 30-89 mL/minute).1
Capivasertib has not been studied in patients with severe renal impairment (Clcr 15-29 mL/minute).1
The manufacturer makes no specific dosage recommendations for geriatric patients.1
Severe hyperglycemia, including diabetic ketoacidosis and fatal outcomes, has occurred in patients treated with capivasertib.1 The safety of capivasertib has not been established in patients with type 1 diabetes or diabetes requiring insulin.1 Patients with insulin-dependent diabetes were excluded from the CAPItello-291 trial.1
Increased fasting glucose from baseline occurred in 37% of patients treated with capivasertib.1 Grade 2, grade 3, or grade 4 hyperglycemic events occurred in 11%, 2%, and 1.1% of patients, respectively.1 Diabetic ketoacidosis and diabetic metabolic decompensation occurred in 0.3 and 0.6% of patients, respectively.1 Dosage reduction for hyperglycemia was required in 0.6% of patients, and permanent discontinuation was required in 0.6% of patients.1 The median time to first occurrence of hyperglycemia was 15 days (range, 1-367).1
In CAPItello-291, 12% of patients administered capivasertib had an anti-hyperglycemic regimen either initiated or changed during the study, including treatment with insulin in 4.8% of patients.1
Evaluate fasting blood glucose and hemoglobin A1c(HbA1c), and optimize blood glucose prior to treatment.1
After initiating treatment with capivasertib, monitor or self-monitor fasting glucose levels on Day 3 or 4 of the dosing week during weeks 1, 2, 4, 6 and 8; then monthly while on treatment; and as clinically indicated.1 Monitor HbA1C levels every 3 months during treatment and as clinically indicated.1 Patients with a history of well-controlled type 2 diabetes mellitus may require intensified anti-hyperglycemic treatment and close monitoring of fasting glucose levels.1
For patients who experience hyperglycemia during treatment with capivasertib; monitor fasting glucose at least twice weekly, on days on and off therapy, until fasting glucose decreases to baseline levels.1 During treatment with anti-diabetic medications, monitor fasting glucose at least once a week for 2 months, followed by once every 2 weeks, or as clinically indicated.1
Consider consultation with a healthcare practitioner with expertise in the treatment of hyperglycemia and initiation of fasting glucose monitoring at home for patients who have risk factors for hyperglycemia or who experience hyperglycemia.1 Advise patients of the signs and symptoms of hyperglycemia and counsel patients on lifestyle changes.1
Withhold capivasertib immediately when ketoacidosis is suspected.1 If ketoacidosis is confirmed, permanently discontinue therapy.1 Based on the severity of the hyperglycemia, withhold, reduce dose, or permanently discontinue capivasertib.1
Severe diarrhea associated with dehydration has occurred in patients treated with capivasertib.1 Diarrhea occurred in 72% of patients; grade 3 or 4 diarrhea occurred in 9% of patients.1 The median time to first occurrence was 8 days (range, 1-519).1
In patients with diarrhea, 59% required antidiarrheal medications to manage symptoms.1 Dosage reductions of capivasertib were required in 8% of patients, and 2% of patients permanently discontinued capivasertib due to diarrhea.1 In patients with grade 2 or higher diarrhea with ≥1 grade improvement, the median time to improvement from the first event was 4 days (range, 1-154).1
Monitor patients for signs and symptoms of diarrhea.1 Advise patients to increase oral fluids and start antidiarrheal treatment at the first sign of diarrhea while taking capivasertib.1 Withhold, reduce dose, or permanently discontinue capivasertib based on the severity of diarrhea.1
Cutaneous adverse reactions, including severe reactions, have occurred in patients treated with capivasertib; these included erythema multiforme, palmar-plantar erythrodysesthesia, and drug reaction with eosinophilia and systemic symptoms (DRESS).1
Cutaneous adverse reactions occurred in 58% of patients; grade 3 or 4 cutaneous adverse reactions occurred in 17% of patients receiving capivasertib.1 Erythema multiforme and DRESS occurred in 1.7 and 0.3% of patients, respectively.1 Dosage reduction was required in 7% of patients, and 7% of patients permanently discontinued capivasertib due to cutaneous adverse reactions.1
The median time to onset of cutaneous adverse reactions was 13 days (range, 1-575).1 Among the patients with cutaneous adverse reactions, 44% required corticosteroid treatment.1 Of these, 37 and 19% were treated with topical and systemic corticosteroids, respectively.1 In patients with grade 2 or higher cutaneous adverse reactions with ≥1 grade improvement, the median time to improvement from the first event was 12 days (range, 2-544).1
Monitor patients for signs and symptoms of cutaneous adverse reactions.1 Early consultation with a dermatologist is recommended.1 Withhold, reduce dose, or permanently discontinue capivasertib based on reaction severity.1
Fetal/Neonatal Morbidity and Mortality
Based on the mechanism of action of capivasertib and animal findings, the drug may cause fetal harm if administered to pregnant females.1 In an animal reproduction study, oral administration of capivasertib to pregnant rats during organogenesis caused maternal toxicities and adverse developmental outcomes (e.g., embryofetal mortality, reduced fetal weights) at maternal exposures 0.7 times the human exposure (AUC) at the recommended dosage of 400 mg twice daily.1
Verify pregnancy status in females of reproductive potential prior to initiating capivasertib.1 Apprise pregnant women and females of reproductive potential of the potential hazard to a fetus.1 Advise females of reproductive potential to use effective contraception during treatment with capivasertib and for 1 month after the last dose.1 Advise males with female partners of reproductive potential to use effective contraception during treatment with capivasertib and for 4 months after the last dose.1
Capivasertib is used in combination with fulvestrant; refer to the full prescribing information of fulvestrant for pregnancy, contraception, and infertility information.1
Capivasertib may cause fetal harm if administered to pregnant females based on its mechanism of action and findings from animal studies.1 Human data on capivasertib use during pregnancy are not available.1 Oral administration of capivasertib to pregnant rats during the period of organogenesis resulted in maternal toxicities (reduced body weight gain and food consumption, increased blood glucose) and adverse developmental outcomes (e.g., post-implantation loss, reduced fetal weights, minor fetal visceral variations) at maternal exposures 0.7 times the human exposure (AUC) at the recommended dose of 400 mg twice daily.1
Verify pregnancy status in females of reproductive potential prior to initiating capivasertib.1 Apprise pregnant women and females of reproductive potential of the potential hazard to a fetus.1
It is unknown whether capivasertib or its metabolites distribute into human milk, or affect milk production or the breast-fed child.1 Capivasertib was detected in the plasma of suckling rat pups.1
Because of the potential for serious adverse reactions to capivasertib in breast-fed children, advise women not to breast-feed during treatment with capivasertib.1
Capivasertib is used in combination with fulvestrant; refer to the full prescribing information of fulvestrant for lactation information.1
Females and Males of Reproductive Potential
Capivasertib can cause fetal harm when administered to pregnant women.1 Capivasertib may impair male fertility based on findings in animal studies; effects on female fertility have not been not studied in animals.1
Verify pregnancy status in females of reproductive potential prior to initiating capivasertib.1 Advise females of reproductive potential to use effective contraception during treatment with capivasertib and for 1 month after the last dose.1 Advise males with female partners of reproductive potential to use effective contraception during treatment with capivasertib and for 4 months after the last dose.1
The safety and effectiveness of capivasertib have not been established in pediatric patients.1
In the CAPItello-291 study, 32% of patients were ≥65 years of age while 7% were ≥75 years of age.1 No overall differences in efficacy were observed between geriatric patients ≥65 years of age and younger adults.1 However, safety analysis of capivasertib comparing patients ≥65 years of age to younger adults suggests a higher incidence of grade 3-5 adverse reactions (57% versus 36%), dosage reductions (30% versus 15%), dose interruptions (57% versus 30%), and permanent discontinuations (23% versus 8%), respectively.1
No clinically important differences in capivasertib pharmacokinetics were observed in mild hepatic impairment (bilirubin less than or equal to upper limit of normal [ULN] and AST greater than ULN, or bilirubin >1-1.5 times ULN).1
The effect of moderate hepatic impairment (bilirubin >1.5-3 times ULN and any AST) is not fully characterized.1 Monitor patients with moderate hepatic impairment for adverse reactions due to potential increased capivasertib exposure.1
Capivasertib has not been studied in patients with severe hepatic impairment (bilirubin >3 times ULN and any AST).1
No clinically important differences in capivasertib pharmacokinetics were observed in mild or moderate renal impairment (creatinine clearance [Clcr] 30-89 mL/minute).1
Capivasertib has not been studied in patients with severe renal impairment (Clcr 15-29 mL/minute).1
Adverse effects reported in ≥20% of patients receiving capivasertib include diarrhea, cutaneous adverse reactions, increased random glucose, decreased lymphocytes, decreased hemoglobin, increased fasting glucose, nausea, fatigue, decreased leukocytes, increased triglycerides, decreased neutrophils, increased creatinine, vomiting, and stomatitis.1
Capivasertib is primarily metabolized by cytochrome P-450 (CYP) isoenzyme 3A4 and UDP-glycosyltransferase (UGT) 2B7.1 Capivasertib is a CYP3A substrate.1
In vitro, capivasertib inhibits breast cancer resistance protein (BCRP), organic anion transporting polypeptide (OATP) 1B1, OATP1B3, organic anion transporter (OAT) 3, multidrug and toxin extrusion (MATE) transporter 1, MATE2-K, and organic cation transporter (OCT) 2.1
Drugs Affecting or Affected by Hepatic Microsomal Enzymes
Concomitant use of capivasertib with strong CYP3A inhibitors increases capivasertib exposure, which may increase the risk of capivasertib adverse reactions.1
Itraconazole, a strong CYP3A4 inhibitor, is predicted to increase capivasertib AUC by up to 1.7-fold and peak plasma concentration by up to 1.4-fold.1
Avoid concomitant use with a strong CYP3A inhibitor. 1
If concomitant use cannot be avoided, reduce the dose of capivasertib to 320 mg orally twice daily for 4 days followed by 3 days off, and monitor patients for adverse reactions.1 After discontinuation of a strong CYP3A inhibitor, resume the capivasertib dosage (after 3-5 half-lives of the inhibitor) that was taken prior to initiating the strong CYP3A inhibitor.1
Concomitant use of capivasertib with moderate CYP3A inhibitors increases capivasertib exposure, which may increase the risk of capivasertib adverse reactions.1
Erythromycin and verapamil, moderate CYP3A inhibitors, are predicted to increase capivasertib AUC by up to 1.5-fold and peak plasma concentration by up to 1.3-fold.1
When concomitantly used with a moderate CYP3A inhibitor, reduce the dose of capivasertib to 320 mg orally twice daily for 4 days followed by 3 days off, and monitor patients for adverse reactions.1 After discontinuation of a moderate CYP3A inhibitor, resume the capivasertib dosage (after 3-5 half-lives of the inhibitor) that was taken prior to initiating the moderate CYP3A inhibitor1
Strong or Moderate CYP3A Inducers
Concomitant use of capivasertib with strong or moderate CYP3A inducers decreases capivasertib exposure, which may reduce the effectiveness of capivasertib.1
Rifampicin, a strong CYP3A4 inducer, is predicted to decrease capivasertib AUC by 70% and peak plasma concentration by 60%.1
Efavirenz, a moderate CYP3A4 inducer, is predicted to decrease capivasertib AUC by 60% and peak plasma concentration by 50%.1
Avoid concomitant use of capivasertib with strong or moderate CYP3A inducers.1
Concomitant use of capivasertib and desipramine, a CYP2D6 substrate, is predicted to increase desipramine AUC by up to 2.1-fold on day 4.1
Concomitant use of capivasertib and midazolam, a CYP3A substrate, increased midazolam AUC by 1.8-fold on day 4 and by 1.2-fold on day 7.1
No clinically important differences in capivasertib pharmacokinetics are predicted when used concomitantly with probenecid, a UGT2B7 inhibitor.1
No clinically important differences in capivasertib pharmacokinetics were observed with concomitant use of capivasertib and rabeprazole.1
Concomitant use of capivasertib and raltegravir, a UGT1A1 substrate, is predicted to increase raltegravir AUC by up to 1.7-fold on day 4.1
No clinically important differences in the pharmacokinetics of warfarin, a CYP2C9 substrate, are predicted when used concomitantly with capivasertib.1
Capivasertib is a kinase inhibitor.1 Capivasertib inhibits all 3 isoforms of serine/threonine kinase AKT (AKT1, AKT2, AKT3) and phosphorylation of downstream AKT substrates.1 AKT activation in tumors occurs due to activation of upstream signaling pathways, mutations in AKT1 , loss of phosphatase and tensin homolog (PTEN) function, and mutations in the catalytic subunit alpha of phosphatidylinositol 3-kinase ( PIK3CA ).1 In vitro, capivasertib reduced growth of breast cancer cell lines including those with relevant PIK3CA or AKT1 mutations or PTEN alteration.1 In vivo, capivasertib alone and in combination with fulvestrant inhibited tumor growth of mouse xenograft models including estrogen-receptor positive breast cancer models with alterations in PIK3CA , AKT1 , and PTEN .1
The absolute bioavailability of capivasertib is 29%.1 The time to peak plasma concentration of capivasertib is approximately 1-2 hours.1 When administered with a high-fat meal (approximately 1000 kcal; fat 60%) or a low-fat meal (approximately 400 kcal; fat 26%), no clinically important differences in capivasertib pharmacokinetics were observed.1 Steady-state concentrations of capivasertib are predicted to be attained on the third and fourth dosing day of each week, starting at week 2.1 Capivasertib plasma concentrations are approximately 0.5-15% of the steady-state peak plasma concentrations during off-dosing days.1 Capivasertib AUC and peak plasma concentrations are dose-proportional over a dosage range of 80-800 mg (0.2-2 times the approved recommended dosage).1
Capivasertib plasma protein binding is 22% and the plasma-to-blood ratio is 0.71.1 Capivasertib is primarily metabolized by cytochrome P-450 (CYP) isoenzyme 3A4 and UDP-glycosyltransferase (UGT) 2B7.1 Renal clearance of the drug is 21% of total clearance.1 Following a single radiolabeled oral dose of 400 mg, the mean total recovery was 45% from urine and 50% from feces.1 The half-life of capivasertib is 8.3 hours.1 No clinically important differences in capivasertib pharmacokinetics have been observed based on age (26-87 years), sex (88% females), race/ethnicity (white, Asian, Black, American Indian or Alaskan Native, and Native Hawaiian or Other Pacific Islander), or body weight (32-150 kg).1
Additional Information
The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care. For further information on the handling of antineoplastic agents, see the ASHP Guidelines on Handling Hazardous Drugs at [Web].
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Capivasertib is available through specialty pharmacies and specialty distributors.4 Consult the Truqap®website ([Web]) for specific availability information.4
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Tablets, film-coated | 160 mg | Truqap® | AstraZeneca |
200 mg | Truqap® | AstraZeneca |
AHFS® Drug Information. © Copyright, 1959-2026, Selected Revisions June 10, 2025. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
Only references cited for selected revisions after 1984 are available electronically.
1. AstraZeneca Pharmaceuticals LP. TRUQAP® (capivasertib) ORAL prescribing information. 2025 Feb. [Web]
2. Turner NC, Oliveira M, Howell SJ, et al. Capivasertib in hormone receptor-positive advanced breast cancer. N Engl J Med . 2023;388(22):2058-2070.
3. Burstein HJ, DeMichele A, Fallowfield L, et al. Endocrine and targeted therapy for hormone receptor-positive, human epidermal growth factor receptor 2-negative metastatic breast cancer-capivasertib-fulvestrant: ASCO rapid recommendation update. J Clin Oncol . 2024;42(12):1450-1453.
4. Truqap® Access & Support: Acquisition Information. From AstraZeneca for US Healthcare Professionals website. Accessed 2024 Jul 22. [Web]