Adagrasib is an innovative KRASG12C inhibitor, which was first approved for marketing in the United States in 2022. As a major breakthrough in the field of targeted therapy, this medication provides a new treatment option for patients with advanced cancer harboring specific gene mutations.

What Are the Indications of Adagrasib?

Treatment of Non-Small Cell Lung Cancer (NSCLC)

Adagrasib is used as a monotherapy.

It is indicated for adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) confirmed to have KRASG12C mutation by an FDA-approved detection method, and these patients have received at least one prior systemic therapy.

Combined Treatment of Colorectal Cancer (CRC)

In the field of colorectal cancer, adagrasib is used in combination with cetuximab.

It is indicated for adult patients with locally advanced or metastatic colorectal cancer (CRC) confirmed to have KRASG12C mutation by an FDA-approved detection method.

And these patients have previously received chemotherapy regimens containing fluoropyrimidines, oxaliplatin, and irinotecan.

Specifications and Properties of Adagrasib

Dosage Form Design and Content Standards

Adagrasib is supplied as film-coated tablets, with each tablet containing 200 mg of the active ingredient.

The tablets are oval, appearing white to off-white. One side is engraved with the word "200", and the other side is printed with a stylized "M" logo.

Ingredient Composition and Physicochemical Properties

The chemical name of adagrasib, the active ingredient of the medication, is {(2S)-4-[7-(8-chloronaphthalen-1-yl)-2-{[(2S)-1-methylpyrrolidin-2-yl]methoxy}-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl}acetonitrile. Its molecular formula is C₃₂H₃₅ClFN₇O₂, and its molecular weight is 604.1 g/mol.

In terms of excipients, it includes colloidal silicon dioxide, crospovidone, magnesium stearate, mannitol, and microcrystalline cellulose.

The film-coating layer contains hypromellose, maltodextrin, medium-chain triglycerides, polydextrose, talc, and titanium dioxide.

Storage and Stability Management of Adagrasib

Environmental Control Requirements

Adagrasib must be stored at a standard room temperature between 20°C and 25°C (68°F and 77°F), with short-term exposure to temperatures ranging from 15°C to 30°C (59°F to 86°F allowed).

The medication is packaged in white opaque square bottles made of high-density polyethylene, which are equipped with desiccants and polypropylene child-resistant caps with tamper-evident heat-sensitive seals inside.

Packaging Specifications and Operating Standards

Packaging Configuration: Two packaging specifications are available, namely bottles containing 120 tablets and 180 tablets respectively.

Sealing Protection: After use, the bottle cap must be tightly closed immediately, and the desiccant should be kept in place.

Safety Protection: The medication must be stored in a safe area out of the reach of children to prevent accidental ingestion.

Humidity Control: Storing the medication in high-humidity areas such as bathrooms and kitchens is strictly prohibited.

Stability Assurance Measures

The desiccant provided in the medication packaging is crucial for maintaining product quality and must not be removed.

The bottle cap adopts a child-resistant design to ensure medication safety.

The medication should be sealed promptly after each dose is taken to prevent moisture absorption and deterioration.