Cited by 333Lung Cancer Treatments and MutationsCancer Genomics and DiagnosticsLung Cancer Research Studies

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FDA Approval Summary: Sotorasib for KRAS G12C -Mutated Metastatic NSCLC

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Nakajima, Erica C., Drezner, Nicole, Li, Xiaoxue, Mishra-Kalyani, Pallavi S., Liu, Yajun, Zhao, Hong, Bi, Youwei, Liu, Jiang, Rahman, Atiqur, Wearne, Emily, Ojofeitimi, Idara, Hotaki, Lauren Tesh, Spillman, Dianne, Pazdur, Richard, Beaver, Julia A., Singh, Harpreet·2022·Clinical Cancer Research

DOI 10.1158/1078-0432.ccr-21-3074PMC PMC9012672

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Abstract

On May 28, 2021, the FDA granted accelerated approval to sotorasib (Lumakras, Amgen) for the treatment of adults with advanced non–small cell lung cancer (NSCLC) with a Kirsten rat sarcoma proto-oncogene (KRAS) G12C mutation who have received at least one prior systemic therapy. The approval was based on CodeBreaK 100 (Study 20170543), a dose-escalation and dose-expansion trial in patients with an advanced, KRAS G12C-mutated, solid tumor. The overall response rate (ORR) observed in patients with KRAS G12C-mutated NSCLC treated with sotorasib (n = 124) was 36% [95% confidence interval (CI), 28–45]. The median duration of response was 10.0 months (95% CI, 6.9–not estimable). The most common adverse reactions (≥20%) were diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, and cough. This is the first approval of a targeted therapy for KRAS G12C-mutated NSCLC. Because of pharmacokinetic data and ORRs of patient cohorts who took sotorasib at lower doses in the dose-escalation portion of CodeBreaK 100, a dose comparison study is being conducted as a post-marketing requirement.

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BackgroundInfluential
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Background
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Background
High-sensitivity label-free electrochemical genosensors for carbon nanotube plasmon-assisted detection of somatic mutations in nucleic acids from formalin-fixed paraffin-embedded tissues
Егорова, В. П., Grushevskaya, H. V., Крылова, Н. Г., Васьковцев, Е. В., Babenka, A. S., Anufreyonak, I. V., Smirnov, S., & Krylov, G. G. (2024) · Microchemical Journal · doi:10.1016/j.microc.2024.112234 · Cited by 6
Exploiting 19F NMR in a Multiplexed Assay for Small GTPase Activity
Bhinderwala, F., & Gronenborn, A. M. (2024) · Journal of the American Chemical Society · doi:10.1021/jacs.4c14294 · Cited by 6
Structural insights, regulation, and recent advances of RAS inhibitors in the MAPK signaling cascade: a medicinal chemistry perspective
Prajapati, V., Singh, A. K., Kumar, A. M., Singh, H., Pathak, P., Grishina, M., Kumar, V., Khalilullah, H., Verma, A., & Kumar, P. (2025) · RSC Medicinal Chemistry · doi:10.1039/d4md00923a · Cited by 6
Self-citation
Wild-type RAS signaling is an essential therapeutic target in RAS -mutated cancers
Sealover, N. E., Finniff, B. A., Hughes, J. M., Sheffels, E., Lee, H., LaMorte, J. P., Gambhir, V., Beckley, Z., Linke, A. J., Wilkerson, M. D., et al. (2025) · Science Signaling · doi:10.1126/scisignal.adx5186 · Cited by 7
Prognostic and Predictive Biomarkers in Head and Neck Squamous Cell Carcinoma Treated with Radiotherapy—A Systematic Review
Schanne, D. H., Koch, A., Eliçin, O., Giger, R., Medová, M., Zimmer, Y., & Aebersold, D. M. (2022) · Biomedicines · doi:10.3390/biomedicines10123288 · Cited by 7
“A clinically approved treatment targeting this mutation in non-small cell lung cancer (NSCLC) [36] is available but unfortunately, the respective publication in our analysis did not indicate the specific KRAS mutation linked to the reported worse LRC. Prevalence of the G12C mutation has been estimated to be 0.24% in H…”
ResultInfluential
A real-world pharmacovigilance study of KRAS G12C mutation inhibitors based on the food and drug administration adverse event reporting system
Wu, L., Xu, M., Li, X., Aierken, D., Yu, J., & Qin, T. (2024) · Frontiers in Pharmacology · doi:10.3389/fphar.2024.1418469 · Cited by 6
Self-citation
Synthetic approaches and clinical application of KRAS inhibitors for cancer therapy
Jiang, M., Ma, S., Xuan, Y., & Chen, K. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117626 · Cited by 6
Augmenting precision medicine via targeted RNA-Seq detection of expressed mutations
Li, D., Li, J., Johann, D. J., Butler, D., Chen, G., Foox, J., Gong, B., Jones, W. D., Kreil, D. P., Kusko, R. L., et al. (2025) · npj Precision Oncology · doi:10.1038/s41698-025-00993-8 · Cited by 6
“Numerous other targeted therapies addressing various KRAS mutations are in clinical development 35 – 38 .”
Survival of patients with KRAS G12C mutated stage IV non-small cell lung cancer with and without brain metastases treated with immune checkpoint inhibitors
Swart, E. M., Noordhof, A. L., Damhuis, R. A. M., Kunst, P. W. A., Ruysscher, D. D., Hendriks, L. E. L., van Geffen, W. H., & Aarts, M. J. (2023) · Lung Cancer · doi:10.1016/j.lungcan.2023.107290 · Cited by 6
Post-marketing safety concerns of sotorasib: A disproportionality analysis based on FDA adverse event reporting system
Ding, Y., Su, H., Shu, Y., & Chen, J. (2024) · Heliyon · doi:10.1016/j.heliyon.2024.e30437 · Cited by 6
“It is used to treat adult patients of locally advanced or metastatic NSCLC with KRAS G12C-mutation who have received at least one previous systemic treatment [3,5].”
Background
Untangling sporadic brain arteriovenous malformations: towards targeting the KRAS/MAPK pathway
Jabarkheel, R., Li, L., Frankfurter, M., Zhang, D. Y., Gajjar, A. A., Muhammad, N., Srinivasan, V. M., Burkhardt, J., & Kahn, M. L. (2024) · Frontiers in Surgery · doi:10.3389/fsurg.2024.1504612 · Cited by 5
“Sotorasib was the ﬁ rst KRAS inhibitor to receive FDA approval for the treatment of KRAS G12C mutated non-small cell lung cancer (88).”
Anti-proteolytic regulation of KRAS by USP9X/NDRG3 in KRAS-driven cancer development
Koo, H., Park, K., Sohn, H., Kang, M.-H., Kim, D. J., Park, Z.-Y., Park, S., Min, S.-H., Park, S.-H., You, Y.-M., et al. (2025) · Nature Communications · doi:10.1038/s41467-024-54476-8 · Cited by 6
“Recently,mutation-speci ﬁ cinhibitorstargetingtheG12C-mutantKRAS have been developed 7,8 , and gained regulatory approval for KRAS-mutant NSCLC (non-small cell lung cancer) patients 9,10 .”
Comprehensive genomic profiling of over 10,000 advanced solid tumors
Jean–Paul De La, O., Hoag, J. R., Deem, A. K., Wang, M., Starodynov, A., Udhane, S. S., Lobello, J. R., Therala, N., Hall, D. W., Basu, G. D., et al. (2025) · Oncotarget · doi:10.18632/oncotarget.28757 · Cited by 5
“Recently, therapies targeting constitutive KRAS activation were shown to extend PFS for patients with NSCLC and CRC harboring KRAS G12C mutations, including adagrasib (CRC and NSCLC) [44, 45] and sotorasib (NSCLC) [46].”
CREPT promotes LUAD progression by enhancing the CDK9 and RNAPII assembly to promote ERK-driven gene transcription
Li, M., Lin, Y.-T., Wang, J., He, Y., Ma, D., Tian, Y., Wang, Y., Liu, Y., Farooq, U., Wang, Y., et al. (2025) · Theranostics · doi:10.7150/thno.115572 · Cited by 5
“Despite this advancement and available drugs developed to target EGFR or KRAS mutations, clinical outcomes have remained unsatisfactory [4].”
Self-citation
Comprehensive molecular landscape of anal squamous cell carcinoma: analysis of tissue and liquid biopsies from 1844 patients
Smolenschi, C., Sisoudiya, S. D., Hollebecque, A., Sivakumar, S., Montesion, M., Euzen, V., Boige, V., Boilève, A., Valéry, M., Sourouille, I., et al. (2025) · npj Precision Oncology · doi:10.1038/s41698-025-01181-4 · Cited by 5
“G12C inhibitors have now been FDA-approved for NSCLC and colorectal cancer, and our ﬁ ndings suggest that these inhibitors should also be evaluated for aSCC 47,48 .”
Therapeutic strategies for KRAS G12C-mutant non-small cell lung cancer: from bench to bedside and beyond
Huang, R., Gong, X., Du, J., Xu, G., Qian, J., Liao, G., Lin, Y., Pan, M., Zheng, B., Yuan, W., et al. (2026) · Frontiers in Pharmacology · doi:10.3389/fphar.2025.1704347 · Cited by 6
Expanding landscape of kinase inhibitor research in 25 years (2001-2025) and advancements of next-generation kinase inhibitors
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Targeting KRAS-G12C in lung cancer: The emerging role of PROTACs in overcoming resistance
Chidambaram, K., Rekha, A., Goyal, A., & Rana, M. (2025) · Pathology - Research and Practice · doi:10.1016/j.prp.2025.155954 · Cited by 5
Precision diagnostics in cancer: Predict, prevent, and personalize
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Developing an effective quality evaluation strategy of next-generation sequencing for accurate detecting non-small cell lung cancer samples with variable characteristics: a real-world clinical practice
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Targeted Therapies in the Most Common Advanced Solid Tumors, Drug Resistance, and Counteracting Progressive Micrometastatic Disease: The Next Frontier of Research
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“Currently, PBC and/or immune checkpoint inhibitors (ICIs) represent standard treatment options for advanced NSCLC lacking EGFR or ALK alterations [34].”
An evaluation of sotorasib for the treatment of patients with non–small cell lung cancer with KRASG12C mutations
Strohbehn, G. W., Sankar, K. N., Qin, A., & Kalemkerian, G. P. (2022) · Expert Opinion on Pharmacotherapy · doi:10.1080/14656566.2022.2134777 · Cited by 5
“Interestingly, systemic drug exposure with repetitive dosing, as measured by peak plasma concentration and AUC0-24h, was not significantly affected by dose over the clinically relevant dose range of 180–960 mg daily [31].”
Background
The Role of Targeted Therapy in the Multi-Disciplinary Approach to Colorectal Liver Metastasis
Ruff, S. M., Shannon, A. H., & Pawlik, T. M. (2023) · Cancers · doi:10.3390/cancers15133513 · Cited by 5
“Both were recently approved by the FDA for use in non-small cell lung cancer [106,107].”
Background
Validated LC-MS/MS method for simultaneous quantification of KRASG12C inhibitor sotorasib and its major circulating metabolite (M24) in mouse matrices and its application in a mouse pharmacokinetic study
Retmana, I. A., Loos, N. H. C., Schinkel, A. H., Beijnen, J. H., & Sparidans, R. W. (2023) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2023.115612 · Cited by 5
Vaccine antibodies against a synthetic epidermal growth factor variant enhance the antitumor effects of inhibitors targeting the MAPK/ERK and PI3K/Akt pathways
García-Román, S., Garzón‐Ibáñez, M., Bertrán-Alamillo, J., Jordana‐Ariza, N., Giménez-Capitán, A. A., García‐Peláez, B., Vives-Usano, M., Codony‐Servat, J., d'Hondt, E., Rosell, R., et al. (2024) · Translational Oncology · doi:10.1016/j.tranon.2024.101878 · Cited by 4
“More recently, KRAS inhibitors targeting specific hotspot mutations have been developed and two of them, adagrasib and sotorasib, have received fast-track approval for treatment of G12C KRAS -mut NSCLC [10,11].”
Off-target engagement of sotorasib with PPARγ via FABP4: a novel mechanism driving interstitial lung disease
Zhang, J., Li, J., Cheng, M., Zhou, H., Zhang, X., Yan, H., Xu, Z., Yang, B., He, Q., Gao, Z., et al. (2025) · Cell Communication and Signaling · doi:10.1186/s12964-025-02425-3 · Cited by 4
El cáncer de pulmón de células no pequeñas en la era de la medicina de precisión
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Does artificial intelligence need companionship to assist in drug discovery? The Kirsten rat sarcoma virus study
Stitou, M., Koomen, J. M., Imbody, D. J., Liao, Y., Monastyrskyi, A., Rix, U., Duckett, D. R., Haura, E. B., & Karolak, A. M. (2024) · BJR|Artificial Intelligence · doi:10.1093/bjrai/ubae001 · Cited by 3
MEK Inhibition in a Pilocytic Astrocytoma With a Rare KRAS Q61R Mutation in a Young Adult Patient: A Case Report
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Recent Advancement in Drug Designing as Small Molecules in Targeted Cancer Therapy: Challenges and Future Directions
Prakash, S., Tyagi, P., Singh, P., Rajkumar, R., & Singh, A. P. (2024) · Current Cancer Drug Targets · doi:10.2174/0115680096331827240911165227 · Cited by 8
Stratification of patients with KRAS-mutated advanced non-small cell lung cancer: improving prognostics
Zhang, Y., Zeng, F., Peng, S., Chen, Y., Jiang, W., Wang, Z., Li, D., Huang, Z., Qin, H., Yan, H., et al. (2023) · Expert Review of Respiratory Medicine · doi:10.1080/17476348.2023.2265810 · Cited by 4
“Sotorasib, which directly targets the KRAS site by blocking the mutant protein’s activity, has been approved by the FDA for treating KRAS-mutated NSCLC [83].”
Background
Sotorasib as first-line therapy in patients with advanced non-small cell lung cancer with KRAS gene mutations combined with brain metastases: a case report
Jia, X., Liu, M., & Cheng, Z. (2024) · AME Case Reports · doi:10.21037/acr-23-153 · Cited by 4
“The most common adverse events reported with sotorasib were pneumonia, hepatotoxicity, and diarrhea (9).”
BIreactive: Expanding the Scope of Reactivity Predictions to Propynamides
Hermann, M. R., Tautermann, C. S., Sieger, P., Grundl, M. A., & Weber, A. (2023) · Pharmaceuticals · doi:10.3390/ph16010116 · Cited by 4
“In addition, successful screening against KRAS G12C with further optimization cycles led to a clinical candidate, including structure-based design efforts in combination with targeted compound library synthesis [11,12].”
Pharmacological SOS1 inhibitor BI-3406 demonstrates in vivo anti-tumor activity comparable to SOS1 genetic ablation in KRAS mutant tumorsPreprint
Baltanás, F. C., Kramer‐Drauberg, M., García‐Navas, R., Patrucco, E., Petrini, E., Arnhof, H., Juan, A. O.-S., Rodríguez-Ramos, P., Borrajo, J., Calzada, N., et al. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.09.18.613686 · Cited by 4
Exploring the differences in the tumor microenvironment and immuno-oncologic targets in pancreatic ductal adenocarcinomas (PDAC) according to KRAS mutational status
Faber, E. B., Baca, Y., Xiu, J., Walker, P., Manji, G. A., Gholami, S., Saeed, A., Prakash, A., Botta, G. P., Sohal, D. P. S., et al. (2024) · ESMO Gastrointestinal Oncology · doi:10.1016/j.esmogo.2024.100042 · Cited by 3
“3 While our understanding of these resistance mechanisms is incomplete, one clinical nongenetic resistance mechanism activated the YAP1 pathway and transforming growth factor-b -driven TME changes including epithelial-mesenchymal transition and angiogenesis.”
Immunotherapeutic and Targeted Strategies for Managing Brain Metastases from Common Cancer Origins: A State-of-the-Art Review
Podder, V., Bellur, S. S., Margolin, K. A., Advani, P. P., Mahtani, R. L., Subbiah, V., Novo, G. B., Ranjan, T., & Ahluwalia, M. S. (2024) · Current Oncology Reports · doi:10.1007/s11912-024-01593-8 · Cited by 4
“G12C mutated NSCLC, which led to accelerated drug approval, although the results must be interpreted cautiously [40].”
CDCP1-targeting ADC outperforms standard therapies in Ras-mutant pancreatic cancer
Um, Y. J., Noh, H.-D., Cho, J. G., Ko, H., Wi, T. M., Kim, J.-O., & Park, S. G. (2025) · Molecular Therapy Oncology · doi:10.1016/j.omton.2025.201024 · Cited by 2
“8 11 Although AMG510 was the first approved targeted therapeutic for tumors with KRAS mutations, it is not effective in patients with other Ras mutations and has a narrow therapeutic scope, since the KRAS G12C mutation, for instance, accounts for 2% of pancreatic cancer.”
Mechanisms and current advances in treating KRAS-mutated lung cancer
Chao, C. H.-Y., & Di, Y. P. (2025) · Chinese Medical Journal - Pulmonary and Critical Care Medicine · doi:10.1016/j.pccm.2025.08.001 · Cited by 6
“41 By covalently binding to the mutant cysteine residue of the 12th codon, sotorasib is able to lock KRAS in an inactive GDP-bound state and inhibit the signaling and growth of cancer.”
A central research portal for mining pancreatic clinical and molecular datasets and accessing biobanked samples
Oscanoa, J., Ross‐Adams, H., Ullah, A. Z. M. D., Kolvekar, T. S., Sivapalan, L., Gadaleta, E., Thorn, G. J., Abdollahyan, M., Imrali, A., Saad, A. B., et al. (2025) · Translational Oncology · doi:10.1016/j.tranon.2025.102550 · Cited by 3
“However, alterations within genes that are not typically associated with RAS signalling have also been widely identified across KRAS wild-type PDAC tumours, and require further investigation to determine functional relevance[19,24].”
Advances on drug therapy for KRAS-mutant non-small-cell lung cancer
Tian, T., & Li, W. (2026) · Translational Oncology · doi:10.1016/j.tranon.2026.102668 · Cited by 4
“Currently, sotorasib and adagrasib have been approved by FDA as second-line treatments for patients with locally advanced or metastatic NSCLC (mNSCLC)[14,15].”
In Silico Pharmacokinetic and Molecular Docking Studies of Natural Plants against Essential Protein KRAS for Treatment of Pancreatic Cancer
Kappan, M. M., & George, J. (2023) · Journal of Natural Remedies · doi:10.18311/jnr/2023/31947 · Cited by 3
Measured Steps: Navigating the Path of Oligoprogressive Lung Cancer with Targeted and Immunotherapies
Jongbloed, M., Khosla, A. A., Bartolomeo, V., Jatwani, K., Singh, R., Ruysscher, D. D., Hendriks, L. E. L., & Desai, A. P. (2024) · Current Oncology Reports · doi:10.1007/s11912-023-01490-6 · Cited by 3
Prognostic Value of KRAS Mutations in Relation to PDL1 Expression and Immunotherapy Treatment in Adenocarcinoma and Squamous Cell Carcinoma Patients: A Greek Cohort Study
Tsiouda, T., Domvri, K., Boutsikou, E., Bikos, V., Kyrka, K., Papadaki, K., Pezirkianidou, P., Porpodis, Κ., & Cheva, A. (2024) · Journal of Personalized Medicine · doi:10.3390/jpm14050457 · Cited by 3
“…mutation prevalence, it is just one of many factors to consider when analyzing genetic alterations in NSCLC. Recently, sotorasib, formerly AMG 510, a small molecule was approved for 3rd line of treatment in patients with KRAS G12C-mutated NSCLC after previous immunotherapy and/or chemotherapy [36].”
Background
Discovery of novel TANK-Binding Kinase 1 (TBK1) inhibitor against pancreatic ductal adenocarcinoma
Shih, W.-H., Huang, H.-L., HuangFu, W., Lin, T. E., Sung, T.-Y., Li, M., Huang, G., Chang, Y.-W., Yen, S., Hsieh, H., et al. (2024) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2024.137296 · Cited by 3
Current Strategies and Future Dimensions in the Development of KRAS Inhibitors for Targeted Anticancer Therapy
D'Alessio‐Sands, L., Gaynier, J., Michel‐Milian, V., Agbowuro, A. A., & Brackett, C. M. (2025) · Drug Development Research · doi:10.1002/ddr.70042 · Cited by 5
“It was granted accelerated approval in May 2021 for the treatment of NSCLC in adult patients with a KRAS G12C mutation who have received prior treatments with chemotherapy or immunotherapy and failed (non ‐ naive patients) (Nakajima et al. 2022).”
Small molecules for Kirsten rat sarcoma viral oncogene homolog mutant cancers: Past, present, and future
Dong, P., Ni, J., Zheng, X., Wang, M., Yang, M., & Han, H. (2025) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2025.177428 · Cited by 3
Differential unfolded protein response regulation in KRAS silencing sensitive and innately resistant colorectal cancer cells
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“mutant-specific KRAS-targeted therapy was recently approved for the treatment of non-small cell lung cancer patients with G12C mutations 18,19 .”
Improving the Dosing Schedules of Targeted Anticancer Agents
Levêque, D. (2025) · Pharmaceuticals · doi:10.3390/ph18060848 · Cited by 3
“In fact, data from the FDA clearly showed the absence of a dose exposure relationship with a saturation of oral absorption and a comparable kinetic exposure between 180 mg and 960 mg [72].”
Influential
Mechanistic insights into molecular targeted therapy and immunotherapy for lung cancer
Vincent, T., Sakthivel, K. M., Josephine, C. M. R., Prasad, R., Kathirvelan, C., Kumar, P., Saravanan, M., & Rasmi, R. R. (2025) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2025.152204 · Cited by 3

Authors: Nakajima, E. C., Drezner, N., Li, X., Mishra-Kalyani, P. S., Liu, Y., Zhao, H., Bi, Y., Liu, J., Rahman, A., Wearne, E., Ojofeitimi, I., Hotaki, L. T., Spillman, D., Pazdur, R., Beaver, J. A., & Singh, H.
Affiliations: United States Food and Drug Administration (US)
Corresponding author: Nakajima, Erica C.
ORCID: Nakajima, Erica C.
Drezner, Nicole
Li, Xiaoxue
Mishra-Kalyani, Pallavi S.
Zhao, Hong
Bi, Youwei
Liu, Jiang
Wearne, Emily
Ojofeitimi, Idara
Hotaki, Lauren Tesh
Spillman, Dianne
Pazdur, Richard
Beaver, Julia A.
Singh, Harpreet
Venue: Clinical Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2021-12-10
Volume: 28
Issue: 8
Pages: 1482-1486
ISSN: 1078-0432 (ISSN-L)
1557-3265
DOI: 10.1158/1078-0432.ccr-21-3074
PMC: PMC9012672
OpenAlex: W4200034683
Cited by: 333
References: 22
Citations by year: 2026: 45 · 2025: 78 · 2024: 84 · 2023: 85 · 2022: 41
FWCI: 33.96
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Clinical Cancer Research (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: HHS | U.S. Food and Drug Administration
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Genomics and Diagnostics
Health Sciences › Medicine › Oncology › Lung Cancer Research Studies
Keywords: sotorasib, KRAS G12C mutation, metastatic non-small cell lung cancer, accelerated FDA approval, targeted therapy, overall response rate, adverse effects, hepatotoxicity, dose comparison
MeSH terms: Carcinoma, Non-Small-Cell Lung, Humans, Lung Neoplasms, Mutation, Piperazines, Pyridines, Pyrimidines, Proto-Oncogene Proteins p21(ras), Clinical Trials, Phase I as Topic

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FDA Approval Summary: Sotorasib for KRAS G12C -Mutated Metastatic NSCLC

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