Adagrasib

Adagrasib, manufactured by Lucius Pharmaceuticals, is a targeted drug for KRASG12C mutations, and it is the second targeted drug of this type in the world. This drug is mainly used for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with KRASG12C mutations who have received at least one prior systemic therap.

Adagrasib is an oral inhibitor specifically optimized for KRASG12C mutants, bringing new hope to the field of oncology therapy. Here's a closer look at Adagrasib.

1.Main ingredient

Adagrasib

2.Applicable people

Select patients for treatment of locally advanced or metastatic NSCLC with Adagrasib based on the presence of KRAS G12C mutation in plasma or tumor specimens.If no mutation is detected in a plasma specimen, test tumor tissue.

3.Use in Specific Populations

3.1 Pregnancy

There are no available data on the use of Adagrasib in pregnant women. In animal reproduction studies, oral administration of adagrasib to pregnant rats and rabbits during the period of organogenesis did not cause adverse development effects or embryo-fetal lethality at exposures below the human exposure at the recommended dose of 600 mg twice daily (see Data). In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

3.2 Lactation

There are no data on the presence of adagrasib or its metabolites in human milk, the effects on the breastfed child, or on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with Adagrasib and for 1 week after the last dose.

3.3 Females and Males of Reproductive Potential

Based on findings from animal studies, Adagrasib may impair fertility in females and males of reproductive potential.

3.4 Pediatric Use

The safety and effectiveness of Adagrasib has not been established in pediatric patients.

3.5 Geriatric Use

Of 116 patients who received adagrasib 600 mg orally twice daily in KRYSTAL-1, 49% (57 patients) were ≥ 65 years of age. No overall differences in safety or effectiveness were observed between older and younger patients.

4.Storage

Store tablets at room temperature, 20°C to 25°C (68°F to 77°F). Temperature excursions between 15°C and 30°C (59°F to 86°F) are permitted.

5.Pharmacokinetics

The median (min, max) Tmax of adagrasib is approximately 6 (6, 12) hours. Effect of Food No clinically significant differences in the pharmacokinetics of adagrasib were observed following administration of a high-fat and high-calorie meal (containing approximately 900 to 1000 calories, 50% from fat).

FDA,2022.12