Capivasertib

Patients taking strong CYP3A4 inhibitors: Avoid concomitant use. If use cannot be avoided, reduce capivasertib dose to 320 mg bid for 4 days, followed by 3 days. Following the discontinuation of strong CYP3A4 inhibitor, resume the prior capivasertib dose after 3-5 half-lives of the inhibitor.

Patients taking moderate CYP3A4 inhibitors: Reduce capivasertib dose to 320 mg bid for 4 days, followed by 3 days off. Following the discontinuation of moderate CYP3A4 inhibitor, resume the prior capivasertib dose after 3-5 half-lives of the inhibitor.

Capivasertib May be taken with or without food. Avoid grapefruit juice.

Patient with history of diabetes mellitus. Moderate hepatic impairment. Elderly. Pregnancy. Breastfeeding is not recommended during treatment. Concomitant use with strong or moderate CYP3A4 inhibitors.

Significant: Diarrhoea, including severe diarrhoea associated with dehydration; cutaneous adverse drug reactions (e.g. erythema multiforme, palmar-plantar erythrodysaesthesia, drug reaction with eosinophilia and systemic symptoms).
Blood and lymphatic system disorders: Anaemia.
Gastrointestinal disorders: Nausea, vomiting, dysgeusia, stomatitis, dyspepsia.
General disorders and administration site conditions: Fatigue, mucosal inflammation.
Immune system disorders: Hypersensitivity reactions.
Investigations: Increased blood creatinine and glycosylated Hb.
Metabolism and nutrition disorders: Decreased appetite.
Renal and urinary disorders: UTI.
Skin and subcutaneous tissue disorders: Pruritus, dry skin.
Potentially Fatal: Severe hyperglycaemia associated with diabetic ketoacidosis.

PO: Z (Mortality and malformations were observed in animal studies. Use during pregnancy is not recommended by some manufacturers. Consult product literature for specific recommendations.)

Women of childbearing potential and men with female partners of childbearing potential must use effective birth control method during treatment and for at least 4 weeks (women) or 16 weeks (men) after the last dose.

Screen for the presence of ≥1 alterations in PIK3CA, AKT1, and/or PTEN genes in tumour tissue before treatment. Verify pregnancy status in women of childbearing potential before starting treatment. Obtain fasting blood glucose levels and HbA1c before initiation and during treatment. Monitor hepatic function (e.g. bilirubin, ALT, AST) before treatment initiation. Assess for signs or symptoms of cutaneous adverse reactions, diarrhoea, and hyperglycaemia.

Increased exposure with strong CYP3A4 inhibitors (e.g. itraconazole, ketoconazole, boceprevir, clarithromycin, telithromycin, cobicistat, ritonavir, saquinavir, nefazodone) and moderate CYP3A4 inhibitors (e.g. ciprofloxacin, erythromycin, diltiazem, verapamil, ciclosporin, aprepitant, fluvoxamine, fluconazole). Reduced exposure with strong CYP3A4 inducers (e.g. enzalutamide, rifampicin, phenytoin, carbamazepine) and moderate CYP3A4 inducers (e.g. bosentan, lopinavir, modafinil, nafcillin, thioridazine). May increase the plasma concentrations of CYP3A substrates (e.g. midazolam).

Increased exposure with grapefruit or grapefruit juice. Decreased exposure with St. John's wort.

Description:
Mechanism of Action: Capivasertib, an antineoplastic agent, is a potent and selective kinase inhibitor of all 3 isoforms of serine/threonine kinase AKT (AKT1, AKT2, AKT3). It inhibits the phosphorylation of downstream AKT substrates (e.g. glycogen synthase kinase 3-β, proline-rich AKT substrate of 40 kilodaltons). AKT is a pivotal node in the phosphatidylinositol 3-kinase (PI3K) signalling cascade, controlling multiple cellular processes (e.g. cellular survival, proliferation, cell cycle, metabolism, cell migration, gene transcription). Additionally, it reduces the growth of a range of cell lines derived from solid tumours and haematological diseases.
Pharmacokinetics:
Absorption: Rapidly absorbed. Time to peak plasma concentration: Approx 1-2 hours. Bioavailability: 29%.
Distribution: Plasma protein binding: 78%.
Metabolism: Metabolised in the liver mainly by CYP3A4 and UGT2B7 isoenzymes.
Excretion: Via faeces (50%); urine (45%). Elimination half-life: 8.3 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 25227436, Capivasertib. https://pubchem.ncbi.nlm.nih.gov/compound/Capivasertib. Accessed Sept. 25, 2025.

Store below 30°C. Follow applicable procedures for receiving, handling, administration, and disposal.

Targeted Cancer Therapy

L01EX27 - capivasertib ; Belongs to the class of other protein kinase inhibitors. Used in the treatment of cancer.

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