What kind of medicine is adagrasib?

adagrasib (MRTX849) is an oral small molecule covalent KRAS inhibitor.

The Phase I/II KRYSTAL-1 study has demonstrated the efficacy of adagrasib in advanced non-small cell lung cancer (NSCLC), with a median PFS of 11.1 months.

About Adagrasib

Mirati Ther- Adagrasib, a new drug developed by apeutics, received accelerated approval from the U.S. FDA on December 12, 2022. The approved indication is for adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with KRASG12C mutations who have previously received at least one systemic treatment. This is the second FDA-approved targeted therapy for non-small cell lung cancer that directly inhibits the activity of KRAS mutants.

The role of adagrasib

Adagrasib, as a selective targeted covalent inhibitor of KRASG12C, can directly enter the switch- II "pocket" and binds to it, thus reversing KRASG12C's affinity for GDP and GTP, making it easier for KRASG12C to bind to GDP, locking the molecule in its inactive GDP-binding form to block the KRAS-mediated signaling pathway and inhibit tumor cell proliferation.

The efficacy of adagrasib

The safety and efficacy of adagrasib have been verified in phase I and II clinical studies respectively.

Tumor shrinkage has been observed in trials with patients with CRC, NSCLC, and pancreatic cancer. A phase II clinical study showed that the previously treated mutant NSCLC cohort had an ORR of 42.9% and a DCR of 79 5%, the median PFS time was 6.5 months, and the median overall survival (OS) time was 12.6 months; a phase I~II clinical study showed that in a cohort of advanced metastatic CRC who had failed previous first-line treatment, the ORR was 22%, the DCR was 87%, the median PFS time was 5.6 months, and the median OS time was 10.0 months.

Adagrasiib usage and dosage

1. The recommended dose is 600 mg, taken orally twice a day until the disease worsens or unacceptable toxicity occurs.

2. Take KRAZATI at the same time every day, with or without food, and swallow the whole tablet. Do not chew, crush, or split tablets.

3. If vomiting occurs after taking KRAZATI, do not take additional doses. Resume dosing at the next scheduled time.

4. If a dose is accidentally missed and more than 4 hours have passed from the expected administration time, the dose should be skipped. Resume dosing at the next scheduled time.

The above information comes from the U.S. FDA instructions. Patients should strictly follow the dosage and medication time prescribed by the doctor, and be careful to avoid misuse or overdose. If you have any discomfort or questions, you should consult a doctor in time and follow the doctor's instructions.

For more information about adagrasib, please refer to: This article provides detailed information on the usage and dosage of adagrasib.

Adagrasib side effects

The common side effects of adagrasib are nausea, diarrhea, vomiting, fatigue, musculoskeletal pain, liver toxicity, renal damage, edema, dyspnea and decreased appetite. The following are simple treatment measures for common side effects of adagrasiib:

1. Nausea, diarrhea, and vomiting: avoid greasy food, eat more meals in smaller amounts, try to avoid allergenic foods, and maintain adequate hydration. If symptoms persist or worsen, you can consult your doctor whether drug-assisted treatment is needed.

2. Fatigue: Arrange work and rest time reasonably, ensure adequate sleep, moderate exercise, avoid sitting for long periods of time, and maintain a good mentality.

3. Musculoskeletal pain: Avoid strenuous exercise. You can apply hot or cold compresses appropriately. If symptoms persist or worsen, you can consult your doctor whether drug treatment is needed.

4. Hepatotoxicity and renal damage: Take medication strictly according to the doctor's instructions, monitor relevant indicators regularly, avoid drinking alcohol and using other drugs that may be harmful to the liver and kidneys. If any abnormality occurs, seek medical attention in time.

5. Edema: Control salt intake, avoid standing for long periods of time, and do moderate exercise to promote blood circulation. If symptoms are severe, consult a doctor whether drug intervention is needed.

6. Difficulty breathing: Maintain a well-ventilated environment and keep indoor air fresh. If symptoms worsen, seek medical attention immediately.

7. Decreased appetite: Choose foods that are easy to digest and rich in nutrients, eat in moderation, and avoid overeating. You can consult a nutritionist for further advice.

For the above side effects, patients should promptly take corresponding measures according to their personal circumstances, and seek professional advice and treatment from their doctors when necessary. If you have any discomfort or questions during medication, you should communicate with your doctor immediately.

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