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Table 2 Summary of Other KRASG12C inhibitors [35, 56, 59,60,61, 64, 66,67,68,69, 73,74,75,76]

From: The current landscape of using direct inhibitors to target KRASG12C-mutated NSCLC

Agent

Pharmaceutical Company

Clinical Trial (CT)

ORR of CT

DCR of CT

TRAEs

LY3537982

Eli Lilly and Company

Phase I (NCT04956640)

60%

80%

Diarrhea, constipation, fatigue, peripheral edema, nausea, neutropenia

GDC-6036

Genentech

Phase I (NCT04449874)

53.4%

–

Rash, diarrhea, nausea, vomiting, dry skin, and paronychia

D-1553

InvestisBio

Phase I/II (NCT04585035)

40.5%

91.9%

Elevated AST/ALT increased, diarrhea, hypertension, hypokalemia, increased total or conjugated bilirubin, hypothyroidism, and nausea

HBI-2438

Huyabio International

Phase I (NCT05485974)

–

–

–

JDQ443

Novartis

Phase Ib/II (NCT04699188)

41.7%

54.5% (RP2D of 200 mg BID)

–

Fatigue, edema, diarrhea, nausea, vomiting, and peripheral neuropathy

JAB-21822

Jacobio Pharma

Phase I/II (NCT05009329)

70% (400 & 800 mg QD groups)

100% (400 & 800 mg QD groups)

Anemia, total bilirubin increase, and proteinuria

HS-10370

Jiangsu Hansoh Pharmaceutical company

Phase I/II (NCT05367778)

–

–

–

IBI-351 (GFH925)

Innovent Biologics Inc

Phase I/II (NCT05005234)

61.2%

53.3% (RP2D of 600 mg BID)

92.5%

96.7% (RP2D of 600 mg BID)

Anemia, white blood cell count decreased, ALT increases, and pruritus

BI-1823911

Boehringer Ingelheim

Phase I (NCT04973163)

–

–

–

JNJ-74699157

Johnson & Johnson

Phase I (NCT04006301)

–

–

Increased blood creatinine phosphokinase (grade 3–4)

  1. RP2D Recommended phase 2 dose