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Adagrasib is an oral small molecule drug that inhibits the activity of the KRAS protein by covalently binding to the cysteine residue of the mutant protein, fixing it in an inactive state, thereby blocking downstream signaling pathways, inhibiting the proliferation of tumor cells and promoting apoptosis.
1. Generic name :Adagrasib
2. Trade name : KRAZATI™
3. Dosage form : Oral film-coated tablets
4. Main ingredients u 200c:Each tablet contains 200 mg of adagrasib (hydrochloride form)
KRASG12C mutated non-small cell lung cancer (NSCLC) : For the treatment of adult patients with locally advanced or metastatic NSCLC with KRASG12C mutations confirmed by an FDA-approved test, and the patient must have received at least one prior systemic therapy. This indication is accelerated approval based on objective response rate (ORR) and duration of response (DOR), and subsequent confirmatory trials may be required to confirm clinical benefit.
1. Specifications : 200mg/tablet, oval white to off-white film-coated tablets, with "200" engraved on one side and a stylized "M" logo on the other side.
2. Packaging : 120 tablets or 180 tablets per bottle, equipped with child-safe cap and desiccant.
1. Recommended dosage of : 600mg (3 tablets) orally, twice a day, about 12 hours apart, swallow the whole tablet, with food or on an empty stomach.
2. Treatment of missed doses : If you miss a dose for more than 4 hours, skip the dose and take it at the originally planned time next time; there is no need to take another dose after vomiting.
3. Dose adjustment :
First dose reduction of : 400mg (2 tablets) twice a day;
Second dose reduction of c: 600 mg once a day;
Liver injury : moderate (Child-PughB) reduced to 400mg twice a day, severe (Child-PughC) disabled.
1. Gastrointestinal reactions : 89% of patients experienced nausea, diarrhea or vomiting, and 9% were grade 3-4. Antiemetics and antidiarrheals need to be prepared.
2. QT interval prolongation : Avoid combined use of other QT prolonging drugs, and monitor electrocardiogram and electrolytes before and during treatment.
3. Hepatotoxicity : 32% of patients experienced elevated ALT/AST. Liver function was monitored before treatment and every month for the first 3 months.
4. Interstitial lung disease (ILD) : 4.1% of patients developed ILD/pneumonitis, and the drug must be discontinued immediately if new respiratory symptoms occur.
1. Pregnant women: : Disabled, animal experiments show potential embryotoxicity.
2. Lactation : Breastfeeding is prohibited during treatment and within 1 week of drug withdrawal.
3. Children : Safety has not been established.
4. U200c for the elderly: No dose adjustment is required, but close monitoring is required.
1. Common (≥25%) : Nausea (70%), diarrhea (69%), vomiting (57%), fatigue (55%), musculoskeletal pain (38%), liver toxicity (37%), renal damage (33%).
2. Severe reactions :ILD/pneumonia (4.1%, including fatal cases), QT prolongation (6%), liver damage (0.3% drug-induced hepatitis).
There are no absolute contraindications, but it is contraindicated in severe liver damage (Child-PughC) and in combination with strong CYP3A inducers or sensitive CYP3A substrates.
1. Strong CYP3A inducers (such as rifampicin) : Avoid combined use, which can reduce adagrasiib exposure by 95%.
2. Sensitive CYP3A substrates (such as midazolam) : Combined use will increase the AUC of the substrate by 31 times and should be avoided.
3. QT prolonging drug : Combination use is prohibited as it may increase the risk of arrhythmia.
Save at room temperature (20-25°C). The original bottle should be protected from light and moisture. The desiccant cannot be taken out or swallowed.