Single-Agent Divarasib in Patients With <i>KRAS G12C</i> –Positive Non–Small Cell Lung Cancer: Long-Term Follow-Up of a Phase I Study

A Adrian G. Sacher W Wilson H. Miller (Department of Medicine, Division of Oncology, Jewish General Hospital, Montreal, QC, Canada) M Manish R. Patel L Luis Paz-Ares (Hospital Universitario 12 de Octubre, Universidad Complutense de Madrid, Madrid) J Jia Luo M Maria de Miguel (START Madrid CIOCC Hospital HM Sanchinarro, Madrid, Spain) G Guzman Alonso J João Daniel Guedes (Hospital de Base de São José do Rio Preto, São José do Rio Preto, Brazil) S Se Hyun Kim M Matthew G. Krebs S Scott A. Laurie (Ottawa Hospital Research Institute, Ottawa, ON, Canada) A Alessio Amatu T Ting Qi K Kalpesh Koli (Genentech, Inc, South San Francisco, CA) M Mariah C. Mayo (Genentech, Inc, South San Francisco, CA) S Samantha Bowyer (Department of Medical Oncology, Sir Charles Gairdner Hospital, Nedlands, Australia) R Rasha Cosman J Jayesh Desai (Peter MacCallum Cancer Centre, Melbourne, VIC, Australia) B Ben Markman (Alfred Health and Monash University, Melbourne, VIC, Australia) P Pierre Freres (University Hospital of Liege, Liege, Belgium) M Marc Lambrechts H Hans Prenen C Carlos Barrios (Latin American Cooperative Oncology Group, Porto Alegre, Brazil) J Joao Daniel Cardoso Guedes S Sérgio de Azevedo R Rita De Cassia Costamilan C Carolina Gomes Jacobina Silva T Tabatha Nakakogue Dallagnol S Scott Laurie W Wilson Miller A Adrian Sacher I István Láng I István Takács R Ravit Geva (Department of Radiation Oncology, Tel-Aviv Sourasky Medical Center, Tel Aviv, Israel) R Ruth Perets (Rambam Medical Center and Technion-Israel Institute of Technology, Haifa, Israel) E Einat Shacham-Shmueli (Institute of Oncology, Sheba Medical Center, Ramat Gan, Israel) C Chiara Cremolini G Gianluca Del Conte A Angelo Delmonte A Armando Santoro (IRCCS Humanitas Research Hospital, Milan) S Salvatore Siena M Mansoor Saleh M Myung-Ju Ahn (Department of Hematology and Oncology, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, South Korea) S Sae-Won Han (Seoul National University Hospital and Seoul National University Cancer Research Institute, Seoul, Republic of Korea) T Tae Won Kim (Asan Medical Center, University of Ulsan College of Medicine, Seoul, South Korea) J Jong-Seok Lee H Hans Gelderblom E Eelke Gort L Loes Latten-Jansen M Marloes Van Dongen (Netherlands Cancer Institute, Amsterdam, Netherlands) S Sanjeev Deva (Department of Cancer Sciences, University of Auckland, Auckland, New Zealand) R Rajiv Kumar Øystein Fløtten T Tormod Guren R Rafal Dziadziuszko (Faculty of Medicine, Department of Oncology and Radiotherapy, Medical University of Gdańsk, Gdánsk, Poland) J Jacek Mackiewicz (Cancer Genetic Laboratory, Greater Poland Cancer Centre, Poznan, Poland) R Rafal Stec R Rustem Safin A Andres Cervantes Ruizperez M Maria de Miguel Luken A Alejandro Falcon (Hospital Universitario Virgen del Rocio, Sevilla, Spain) E Elena Garralda Cabanas L Laura Medina (Viver Health, LLC, Morristown, NJ) V Víctor Moreno L Luis Paz-Ares Rodríguez (Department of Medical Oncology, Hospital Universitario 12 de Octubre, Madrid) C Christian Britschgi E Eugenio Fernandez S Simon Häfliger S Sacha Rothschild M Martin Forster R Robert Jones (University of Glasgow, Beatson West of Scotland Cancer Centre, Glasgow, United Kingdom) M Matthew Krebs R Raid Aljumaily K Kathryn Arbor L Lyudmila Bazhenova (University of California, San Diego, San Diego, CA, US) T Timothy Burns M Michael Cheng T Thomas Karasic P Patricia LoRusso (Yale School of Medicine, New Haven, CT) E Erminia Massarelli (City of Hope—Comprehensive Cancer Center, Duarte, CA) P Pamela Munster S Sai-Hong Ou M Manish Patel K Kenneth K. Yau (Hoffmann-La Roche Limited, Mississauga, Canada) J Junko Aimi J Julie Chang (1University of Wisconsin Carbone Cancer Center, Madison, United States) Y Yoonha Choi (Genentech, Inc, South San Francisco, CA) N Neekesh V. Dharia (Genentech, Inc, South San Francisco, CA) X Xuefeng Hou (16Roche Products Ltd, Welwyn Garden City, United Kingdom) T Tomi Jun (Genentech, Inc, South San Francisco, CA) M Mark T. Lin (Genentech, Inc, South San Francisco, CA) S Sandhya Mandlekar H Huy Ngo N Nina Qi S Stephanie Royer-Joo (Genentech, Inc, South San Francisco, CA) J Jennifer L. Schutzman (Genentech, Inc, South San Francisco, CA) Z Zhen Shi (Department of Chemistry) J Julia Suchomel

Abstract

Divarasib (GDC-6036), an oral, highly potent and selective next-generation KRAS G12C inhibitor, has demonstrated a manageable safety profile and promising antitumor activity in patients with advanced KRAS G12C –positive non–small cell lung cancer (NSCLC). Here, we report long-term (≥1 year) follow-up of single-agent divarasib from the ongoing, open-label, and multicenter phase I study (ClinicalTrials.gov identifier: NCT04449874 ). The primary objective was safety, and the other objectives included preliminary antitumor activity. Overall, 65 patients with advanced KRAS G12C –positive NSCLC received single-agent oral divarasib 50-400 mg once daily and 31 patients (48%) were treated beyond 1 year. Divarasib continued to be well tolerated, and the safety profile beyond 1 year was consistent with the overall safety profile. In patients with measurable disease at baseline across all dose levels (n = 63), the confirmed objective response rate was 55.6% (95% CI, 42.5 to 68.1), and the median duration of response was 18.0 months (95% CI, 11.1 to 24.9). The median progression-free survival was 13.8 months (95% CI, 9.8 to 25.4) in the overall population (N = 65) and 15.3 months (95% CI, 12.3 to 26.1) among patients assigned to the 400-mg dose level (n = 44). With extended follow-up, divarasib demonstrated long-term safety and antitumor activity in patients with advanced KRAS G12C –positive NSCLC.

Article Details

Volume / Issue Vol. 43, Issue 30
Published October 20, 2025
Pages 3249-3253
ISSN 0732-183X
Publisher Lippincott Williams & Wilkins

Journal Info

Journal of Clinical Oncology

Lippincott Williams & Wilkins

ISSN: 0732-183X Health Sciences

Authors (98)

A

Adrian G. Sacher

W

Wilson H. Miller

Department of Medicine, Division of Oncology, Jewish General Hospital, Montreal, QC, Canada

M

Manish R. Patel

L

Luis Paz-Ares

Hospital Universitario 12 de Octubre, Universidad Complutense de Madrid, Madrid

J

Jia Luo

M

Maria de Miguel

START Madrid CIOCC Hospital HM Sanchinarro, Madrid, Spain

G

Guzman Alonso

J

João Daniel Guedes

Hospital de Base de São José do Rio Preto, São José do Rio Preto, Brazil

S

Se Hyun Kim

M

Matthew G. Krebs

S

Scott A. Laurie

Ottawa Hospital Research Institute, Ottawa, ON, Canada

A

Alessio Amatu

T

Ting Qi

K

Kalpesh Koli

Genentech, Inc, South San Francisco, CA

M

Mariah C. Mayo

Genentech, Inc, South San Francisco, CA

S

Samantha Bowyer

Department of Medical Oncology, Sir Charles Gairdner Hospital, Nedlands, Australia

R

Rasha Cosman

J

Jayesh Desai

Peter MacCallum Cancer Centre, Melbourne, VIC, Australia

B

Ben Markman

Alfred Health and Monash University, Melbourne, VIC, Australia

P

Pierre Freres

University Hospital of Liege, Liege, Belgium

M

Marc Lambrechts

H

Hans Prenen

C

Carlos Barrios

Latin American Cooperative Oncology Group, Porto Alegre, Brazil

J

Joao Daniel Cardoso Guedes

S

Sérgio de Azevedo

R

Rita De Cassia Costamilan

C

Carolina Gomes Jacobina Silva

T

Tabatha Nakakogue Dallagnol

S

Scott Laurie

W

Wilson Miller

A

Adrian Sacher

I

István Láng

I

István Takács

R

Ravit Geva

Department of Radiation Oncology, Tel-Aviv Sourasky Medical Center, Tel Aviv, Israel

R

Ruth Perets

Rambam Medical Center and Technion-Israel Institute of Technology, Haifa, Israel

E

Einat Shacham-Shmueli

Institute of Oncology, Sheba Medical Center, Ramat Gan, Israel

C

Chiara Cremolini

G

Gianluca Del Conte

A

Angelo Delmonte

A

Armando Santoro

IRCCS Humanitas Research Hospital, Milan

S

Salvatore Siena

M

Mansoor Saleh

M

Myung-Ju Ahn

Department of Hematology and Oncology, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, South Korea

S

Sae-Won Han

Seoul National University Hospital and Seoul National University Cancer Research Institute, Seoul, Republic of Korea

T

Tae Won Kim

Asan Medical Center, University of Ulsan College of Medicine, Seoul, South Korea

J

Jong-Seok Lee

H

Hans Gelderblom

E

Eelke Gort

L

Loes Latten-Jansen

M

Marloes Van Dongen

Netherlands Cancer Institute, Amsterdam, Netherlands

S

Sanjeev Deva

Department of Cancer Sciences, University of Auckland, Auckland, New Zealand

R

Rajiv Kumar

Øystein Fløtten

T

Tormod Guren

R

Rafal Dziadziuszko

Faculty of Medicine, Department of Oncology and Radiotherapy, Medical University of Gdańsk, Gdánsk, Poland

J

Jacek Mackiewicz

Cancer Genetic Laboratory, Greater Poland Cancer Centre, Poznan, Poland

R

Rafal Stec

R

Rustem Safin

A

Andres Cervantes Ruizperez

M

Maria de Miguel Luken

A

Alejandro Falcon

Hospital Universitario Virgen del Rocio, Sevilla, Spain

E

Elena Garralda Cabanas

L

Laura Medina

Viver Health, LLC, Morristown, NJ

V

Víctor Moreno

L

Luis Paz-Ares Rodríguez

Department of Medical Oncology, Hospital Universitario 12 de Octubre, Madrid

C

Christian Britschgi

E

Eugenio Fernandez

S

Simon Häfliger

S

Sacha Rothschild

M

Martin Forster

R

Robert Jones

University of Glasgow, Beatson West of Scotland Cancer Centre, Glasgow, United Kingdom

M

Matthew Krebs

R

Raid Aljumaily

K

Kathryn Arbor

L

Lyudmila Bazhenova

University of California, San Diego, San Diego, CA, US

T

Timothy Burns

M

Michael Cheng

T

Thomas Karasic

P

Patricia LoRusso

Yale School of Medicine, New Haven, CT

E

Erminia Massarelli

City of Hope—Comprehensive Cancer Center, Duarte, CA

P

Pamela Munster

S

Sai-Hong Ou

M

Manish Patel

K

Kenneth K. Yau

Hoffmann-La Roche Limited, Mississauga, Canada

J

Junko Aimi

J

Julie Chang

1University of Wisconsin Carbone Cancer Center, Madison, United States

Y

Yoonha Choi

Genentech, Inc, South San Francisco, CA

N

Neekesh V. Dharia

Genentech, Inc, South San Francisco, CA

X

Xuefeng Hou

16Roche Products Ltd, Welwyn Garden City, United Kingdom

T

Tomi Jun

Genentech, Inc, South San Francisco, CA

M

Mark T. Lin

Genentech, Inc, South San Francisco, CA

S

Sandhya Mandlekar

H

Huy Ngo

N

Nina Qi

S

Stephanie Royer-Joo

Genentech, Inc, South San Francisco, CA

J

Jennifer L. Schutzman

Genentech, Inc, South San Francisco, CA

Z

Zhen Shi

Department of Chemistry

J

Julia Suchomel