I. Basic Information

Generic Name: Capivasertib

Approved Name in China: Capivasertib Tablets

Brand Names: Truqap, CAPIVADX, Quankede

Dosage Forms and Strengths: 160 mg/tablet, 200 mg/tablet; 64 tablets/bottle

Manufacturer: BigBear Pharmaceutical Co., Ltd. (Laos)

Approval No. (Laos FDA) for 160 mg: 12L 1267/24

Approval No. (Laos FDA) for 200 mg: 12L 1269/24

Storage Conditions: 20°C–25°C (excursions permitted between 15°C–30°C during short-term transport); protect from moisture.

II. Indications

Used in combination with fulvestrant for the treatment of locally advanced or metastatic breast cancer meeting the following criteria:

Hormone receptor-positive (HR+), HER2-negative;

Confirmed to harbor one of the following gene alterations—*PIK3CA*, *AKT1*, or *PTEN*—as detected by an FDA-approved test;

Has progressed after receiving at least one endocrine-based regimen, or has recurred within 12 months of completing adjuvant therapy.

III. Mechanism of Action

Target: Inhibits all isoforms of the serine/threonine kinase AKT (AKT1/2/3);

Pathway Blockade: Blocks the aberrant activation of the PI3K/AKT signaling pathway, thereby inhibiting tumor growth and survival.

IV. Dosage and Administration

Dosing Regimen

Recommended Dose: 400 mg (2 tablets), taken orally twice daily (approximately 12 hours apart);

Cycle: Take continuously for 4 days → discontinue for 3 days (weekly cycle);

Administration: Swallow tablets whole (do not chew or crush); may be taken with or without food. #Dosage Adjustment

Dose Reduction for Adverse Reactions:

| Severity | Recommended Action

| Grade 3 Hyperglycemia/Diarrhea/Rash | Suspend treatment → Upon recovery, reduce dose to 320 mg per dose

| Grade 4 or Intolerable Toxicity | Permanently discontinue treatment

Dosage Adjustment for Drug Interactions:

Strong CYP3A Inhibitors (e.g., Clarithromycin): Avoid concomitant use; if necessary, reduce dose to 200 mg per dose;

Moderate CYP3A Inhibitors (e.g., Diltiazem): Reduce dose to 320 mg per dose;

CYP3A Inducers (e.g., Rifampin): Completely avoid concomitant use.

V. Management of Adverse Reactions

Adverse Reactions with an Incidence of ≥20%

Common: Diarrhea (72%), Skin reactions (58%), Hyperglycemia (57%), Lymphocytopenia (47%), Anemia (45%), Nausea (35%), Fatigue (35%).

Laboratory Abnormalities: Increased fasting glucose, increased triglycerides, increased creatinine, decreased neutrophils.

Management of Severe Toxicities

Hyperglycemia:

Monitor blood glucose levels prior to and during treatment; monitor more frequently in patients with diabetes;

Symptoms: Thirst, polyuria, fruity-smelling breath → Seek immediate medical attention.

Diarrhea:

Initiate anti-diarrheal treatment (e.g., Loperamide) at the first sign of symptoms; ensure adequate hydration;

Persists for ≥48 hours or leads to dehydration → Suspend treatment.

Skin Reactions:

Rash, blistering, exfoliation → Reduce dose or discontinue treatment based on severity.

VI. Contraindications and Warnings

Contraindications: Contraindicated in patients with severe hypersensitivity to any component of the product.

Boxed Warning:

Embryo-Fetal Toxicity: May cause fetal harm when administered to pregnant women; effective contraception is required during treatment and for 1 month (for females) or 4 months (for males) after the last dose;

Lactation: Breastfeeding is prohibited during treatment and for 1 month after the last dose. VII. Clinical Efficacy (Key Study: CAPItello-291)

| Patient Population | Median Progression-Free Survival (PFS) | Reduction in Risk of Disease Progression

| Overall Patient Population | 7.2 months vs. 3.6 months (Control Group) | 40% Reduction

| Patients with AKT Pathway Mutations | 7.3 months vs. 3.1 months (Control Group) | >50% Reduction

VIII. Use in Special Populations

Hepatic/Renal Impairment: No definitive dose adjustment recommendations are currently available; close monitoring is required.

Elderly Patients: Safety data for patients aged ≥65 years are limited; individualized assessment is recommended.

IX. Drug Interactions

CYP3A Substrates: Capivasertib is metabolized via CYP3A4; dose adjustments are required when co-administered with CYP3A inhibitors or inducers (see "IV. Dose Adjustments" for details).

Fulvestrant: No known interactions; administer according to the standard regimen.

X. Patient Medication Instructions

Missed Doses: If more than 4 hours remain before the next scheduled dose, take the missed dose; otherwise, skip it. Do not take a double dose.

Monitoring Requirements:

Monitor blood glucose levels weekly (especially for patients with diabetes).

Record the frequency of diarrhea and any changes in skin condition.

Dietary Advice: Avoid grapefruit and grapefruit products (as they inhibit CYP3A).

The information above is based on the drug's prescribing information and Phase III clinical studies. Specific treatment regimens should be formulated by a specialized oncologist based on the individual patient's genetic testing results and tolerability.