Sotorasib (Lumakras)

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Sotorasib is an experimental KRAS inhibitor being investigated for the treatment of KRAS G12C mutant non small cell lung cancer, colorectal cancer, and appendix cancer.

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Sotorasib is an experimental KRAS inhibitor being investigated for the treatment of KRAS G12C mutant non small cell lung cancer, colorectal cancer, and appendix cancer.

Sotorasib, also known as AMG-510, is an acrylamide derived KRAS inhibitor developed by Amgen. It is indicated in the treatment of adult patients with KRAS G12C mutant non small cell lung cancer. This mutation makes up >50% of all KRAS mutations.2 Mutant KRAS discovered in 1982 but was not considered a druggable target until the mid-2010s.5 It is the first experimental KRAS inhibitor.

The drug MRTX849 is also currently being developed and has the same target.

Sotorasib was granted FDA approval on 28 May 2021.

Indication

Sotorasib is indicated in the treatment of adults with KRAS G12C mutant non small cell lung cancer

Pharmacodynamics

Sotorasib is indicated in the treatment of adults with KRAS G12C mutant non small cell lung cancer.6 It has a moderate duration of action as it is given daily.6 Patients should be counselled regarding the risks of hepatotoxicity, interstitial lung disease and pneumonitis; and to avoid breastfeeding during treatment and up to 1 week after the last dose.6

Mechanism of action

Normally GTP binds to KRAS, activating the protein and promoting effectors to the MAP kinase pathway.3 GTP is hydrolyzed to GDP, and KRAS is inactivated.4 KRAS G12C mutations impair hydrolysis of GTP, leaving it in the active form.4

Sotorasib binds to the cysteine residue in KRAS G12C mutations, holding the protein in its inactive form.1 The cysteine residue that sotorasib targets is not present in the wild type KRAS, which prevents off-target effects.6 This mutation is present in 13% of non small cell lung cancer, 3% of colorectal and appendix cancer, and 1-3% of solid tumors.1

TARGET ACTIONS ORGANISM
AGTPase KRas
inhibitor
Humans

Absorption

A 960 mg once daily dose of sotorasib reaches a Cmax of 7.50 µg/mL, with a median Tmax of 2.0 hours, and an AUC0-24h of 65.3 h*µg/mL.5

CHOOSE DOSAGE

120 mg

CHOOSE QUANTITY

20 pills, 50 pills

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