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Capivasertib is an oral small molecule kinase inhibitor that works by targeting the activity of the serine/threonine kinase AKT (including AKT1, AKT2, and AKT3 isoforms).
1. Generic name :Capivasertib
2. Trade name : b>TRUQAP™
3. Dosage form : Oral film-coated tablets
4. Main ingredients : Each tablet contains 160mg or 200mg of capositinib (active ingredient).
HR-positive/HER2-negative advanced breast cancer : Combined with fulvestrant to treat adult patients with locally advanced or metastatic HR-positive/HER2-negative breast cancer carrying PIK3CA/AKT1/PTEN gene alterations, and the patient must have received at least one endocrine therapy for progression in the metastatic disease stage, or relapse within 12 months after adjuvant therapy.
1. Specifications : 160mg (round beige tablets, engraved with "CAV160"); 200mg (capsule-shaped beige tablets, engraved with "CAV200").
2. Packaging : 64 tablets per bottle, equipped with child safety cap.
1. Recommended dosage of : 400mg (2 tablets of 200mg) orally, twice a day (about 12 hours apart), take it for 4 days and then stop taking it for 3 days, and the cycle continues. Can be taken with food or on an empty stomach.
2. Treatment of missed doses : If the missed dose is less than 4 hours, you can take it, and if it exceeds 4 hours, skip it; there is no need to take it after vomiting.
3. Special medication : When used in combination with strong CYP3A inhibitors, the dosage needs to be reduced to 320 mg twice a day.
1. First dose reduction of : 320mg (2 tablets of 160mg) twice a day;
2. Second dose reduction of :200mg twice a day;
3. Permanent discontinuation of : When the second reduction is intolerable.
4. Adjustment basis :
(1) High blood sugar : Pause when fasting blood glucose >250mg/dL, and reduce the dose after recovery; p>
(2). Diarrhea : If grade ≥3, suspend until returning to grade 1;
(3). Skin reaction :Grade ≥3 rash requires suspension or permanent discontinuation.
1. Hyperglycemia monitoring : Test fasting blood sugar and HbA1c regularly before and during treatment. Diabetic patients need to strengthen monitoring.
2. Diarrhea management : 72% of patients have diarrhea. It is recommended to prepare antidiarrheal drugs and increase fluid replenishment.
3. Skin reaction : 58% of patients develop rash. In severe cases, the drug needs to be discontinued and a dermatologist consulted.
4. Dietary taboos : Avoid grapefruit juice (interference with metabolism).
1. Pregnant women: : Disabled (animal experiments show embryotoxicity).
2. Lactation : Breastfeeding is prohibited during treatment and within 1 week of drug withdrawal.
3. U200c liver damage: Moderate to severe (Child-PughB/C) needs to be reduced or disabled.
4. Children : Safety has not been established.
1. Common (≥20%) : Diarrhea (72%), skin reactions (58%), hyperglycemia (57%), lymphopenia (47%), nausea (35%), fatigue (35%).
2. Severe reactions : Grade 3-4 hyperglycemia (2.8%), diarrhea (9%), skin toxicity (17%).
1. Those who are severely allergic to capositinib or excipients;
2. Combined use of strong CYP3A inducers (such as rifampicin).
1. Strong CYP3A inhibitor (such as itraconazole): Need to reduce the dosage to 320 mg twice a day;
2. CYP3A substrate (such as midazolam): may increase the exposure of the latter.
Save at room temperature (20-25°C). The original bottle should be protected from light and moisture.