Sotorasib

LUMAKRAS

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Pronunciation: soe-toe-RAS-ib (LOO-ma-kras)

Sotorasib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Sotorasib ballicule

What it isCovalent KRAS G12C inhibitor; KRAS G12C-mutant non-small-cell lung cancer.

Why this oneIts pocket-binding strategy opened KRAS G12C to direct drug therapy after decades of failure.

What limits itHepatotoxicity and interstitial lung disease require monitoring; gastric acid is needed for absorption, so PPIs interfere.

Sotorasib molecular structure (skeletal formula) — Molecular structure: Sotorasib

FDA-approved for

KRAS G12C-mutated non-small cell lung cancer (2021)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
KRAS G12C-mutated NSCLC (single agent)	Adults	960 mg QD	960 mg QD	960 mg QD
KRAS G12C-mutated mCRC (with panitumumab)	Adults	960 mg QD	960 mg QD	960 mg QD

Renal Undefined

Hepatic Undefined

For mCRC, administer the first LUMAKRAS dose before the first panitumumab infusion

Instructions

Swallow tablets whole with or without food; do not chew, crush, or split
If unable to swallow solids, disperse tablets in 120 mL room-temperature water and drink immediately or within 2 hours
Take at the same time each day
If a dose is missed by more than 6 hours or vomiting occurs, take the next dose the next day
Select patients based on KRAS G12C mutation

Available strengths

tab 120, 240, 320 mg

Cautions

Hepatotoxicity — monitor liver function tests every 3 weeks for first 3 months, then monthly
Interstitial lung disease / pneumonitis

Adverse reactions

Diarrhea
Musculoskeletal pain
Nausea
Fatigue
Hepatotoxicity
Cough (NSCLC)
Rash, dry skin, stomatitis (with panitumumab)
Lab abnormalities (decreased lymphocytes/hemoglobin, increased AST/ALT)

Pregnancy No human data; animal studies showed no major adverse developmental effects up to 4.6× human exposure

Lactation Do not breastfeed during treatment and for 1 week after the last dose

Cost

Sotorasib (LUMAKRAS)

Strength		#/mo	CostPlus
120 mg	tab	30 qd	not offered
240 mg	tab	30 qd	not offered
320 mg	tab	30 qd	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Sotorasib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2040 est.

NO BOXED WARNINGS

Principal riskHepatotoxicity; PPIs reduce absorption

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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