Drug reference

capivasertib

AKT (protein kinase B) inhibitor (antineoplastic)

START

400 mg PO twice daily on 4-on-3-off schedule (with fulvestrant)

TYPICAL MAX

800 mg/day (400 mg BID)

STOP IF

Severe hyperglycaemia / DKA, severe SJS/TEN, or severe diarrhoea

WATCH

HbA1c / glucose, rash, diarrhoea management; PIK3CA/AKT1/PTEN status pre-start

CDSCO approvedATC L01EX27

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · absorption
PEAK: 3h · Tmax
t½: 8h · t½
DURATION: 12h · twice-daily

EXCRETION

Mainly faecal (~50%); ~45% renal

route + CYP

INTERACTIONS

2 major

SEVERE in our sources

PREGNANCY

Can cause fetal harm — avoid; effective contraception during and 1 week after.

FDA category + note

Top interactionssee all 5 →

Strong Cyp3a4 InducersSevereDatabaseKimi deep-research + Cla
Strong Cyp3a4 InhibitorsSevereDatabaseKimi deep-research + Cla

Mechanism

Selective ATP-competitive inhibitor of all three AKT isoforms (AKT1/2/3), blocking PI3K/AKT/mTOR pathway signalling; combined with fulvestrant for HR-positive HER2-negative advanced breast cancer with PIK3CA/AKT1/PTEN alterations.

Indications

HR-positive HER2-negative advanced/metastatic breast cancer with PIK3CA/AKT1/PTEN alterations (with fulvestrant)

Dosing

Adult: 400 mg PO twice daily for 4 days followed by 3 days off (within each 7-day cycle), continued until progression; reduce for toxicity.
Pediatric: Not established.
Renal adjustment: No adjustment for mild–moderate; severe (eGFR <30) not studied.
Hepatic adjustment: Mild: no adjustment; moderate–severe: not studied — caution.
Geriatric: No specific adjustment.
Max dose: 800 mg/day (400 mg BID, 4-on-3-off schedule)

Pharmacokinetics

Onset

Tumour effect over weeks

Peak effect

~2–4 h (Tmax)

Duration

~12 h (twice-daily)

Half-life

~8 h

Bioavailability

Moderate (not significantly food-affected)

Protein binding

~25%

Metabolism

Hepatic CYP3A4 / UGT2B7

Excretion

Mainly faecal (~50%); ~45% renal

Contraindications

Severe hypersensitivity
Caution: diabetes, recent ketoacidosis, infection

Side effects

Common

DiarrhoeaRashHyperglycaemiaNausea/vomitingFatigue

Serious

Severe hyperglycaemia / DKA (rare)
Severe diarrhoea
Severe skin reactions (SJS, TEN)
Embryo-fetal toxicity

Pregnancy & lactation

Pregnancy

Can cause fetal harm — avoid; effective contraception during and 1 week after.

Lactation

Avoid breastfeeding during and 2 weeks after therapy.

Drug interactions

Strong Cyp3a4 Inducers

Severe

Database

Reduced exposure

Avoid combination