NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations

Drilon, Alexander; Horan, Joshua C.; Tangpeerachaikul, Anupong; Besse, Benjamin; Ou, Sai-Hong Ignatius; Gadgeel, Shirish M.; Camidge, D. Ross; van der Wekken, Anthonie J.; Nguyen-Phuong, Linh; Acker, Adam; Keddy, Clare; Nicholson, Katelyn S.; Yoda, Satoshi; Mente, Scot; Sun, Yuting; Soglia, John R.; Kohl, Nancy E.; Porter, James R.; Shair, Matthew D.; Zhu, Viola; Davare, Monika A.; Hata, Aaron N.; Pelish, Henry E.; Lin, Jessica J.

doi:10.1158/2159-8290.cd-22-0968

Cited by 52Lung Cancer Treatments and MutationsCancer Mechanisms and TherapyCancer Genomics and Diagnostics

NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations

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Drilon, Alexander, Horan, Joshua C., Tangpeerachaikul, Anupong, Besse, Benjamin, Ou, Sai-Hong Ignatius, Gadgeel, Shirish M., Camidge, D. Ross, van der Wekken, Anthonie J. +16 more·2023·Cancer Discovery

DOI 10.1158/2159-8290.cd-22-0968PMC PMC9975673

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Abstract

ROS1 tyrosine kinase inhibitors (TKI) have been approved (crizotinib and entrectinib) or explored (lorlatinib, taletrectinib, and repotrectinib) for the treatment of ROS1 fusion–positive cancers, although none of them simultaneously address the need for broad resistance coverage, avoidance of clinically dose-limiting TRK inhibition, and brain penetration. NVL-520 is a rationally designed macrocycle with >50-fold ROS1 selectivity over 98% of the kinome tested. It is active in vitro against diverse ROS1 fusions and resistance mutations and exhibits 10- to 1,000-fold improved potency for the ROS1 G2032R solvent-front mutation over crizotinib, entrectinib, lorlatinib, taletrectinib, and repotrectinib. In vivo, it induces tumor regression in G2032R-inclusive intracranial and patient-derived xenograft models. Importantly, NVL-520 has an ∼100-fold increased potency for ROS1 and ROS1 G2032R over TRK. As a clinical proof of concept, NVL-520 elicited objective tumor responses in three patients with TKI-refractory ROS1 fusion–positive lung cancers, including two with ROS1 G2032R and one with intracranial metastases, with no observed neurologic toxicities. Significance: The combined preclinical features of NVL-520 that include potent targeting of ROS1 and diverse ROS1 resistance mutations, high selectivity for ROS1 G2032R over TRK, and brain penetration mark the development of a distinct ROS1 TKI with the potential to surpass the limitations of earlier-generation TKIs for ROS1 fusion–positive patients. This article is highlighted in the In This Issue feature, p. 517

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ROS1 fusions are rare genetic events reported in multiple solid tumors, including NSCLC, with prevalence 0.9% to 2.6%.
“These ROS1 fusions are rare genetic events reported in multiple solid tumors, including non–small cell lung cancer (NSCLC), where the prevalence is 0.9% to 2.6%.1,3-5”
From Taletrectinib in ROS1 + Non–Small Cell Lung Cancer: TRUST (2025) · cites this paper as [4]

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Safety and preliminary clinical activity of NVL-520, a highly selective ROS1 inhibitor, in patients with advanced ROS1 fusion-positive solid tumors
Drilon, A. E. D. C., Besse, B., Camidge, D. R., Ou, S.-H. I., Gadgeel, S. M., Johnson, M. L., Calles, A., Miguel, M. J. D., Spira, A. I., Felip, E., et al. (2022) · European Journal of Cancer · doi:10.1016/s0959-8049(22)00821-8 · Cited by 12 · see citing works
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Abstract 1465: NUV-520 (NVL-520) is a brain-penetrant and highly selective ROS1 inhibitor with antitumor activity against the G2032R solvent front mutation
Pelish, H. E., Tangpeerachaikul, A., Kohl, N. E., Porter, J. R., Shair, M. D., & Horan, J. C. (2021) · Cancer Research · doi:10.1158/1538-7445.am2021-1465 · Cited by 4 · see citing works
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Abstract 3336: Preclinical activity of NVL-520 in ROS1-driven cancer models with diverse fusion partners and kinase-domain mutations
Tangpeerachaikul, A., Keddy, C., Nicholson, K. S., Davare, M. A., & Pelish, H. E. (2022) · Cancer Research · doi:10.1158/1538-7445.am2022-3336 · Cited by 1 · see citing works
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Abstract LB182: Mutagenesis screens support potential best-in-class profile for selective, brain-penetrant, and TRK-sparing ROS1 inhibitor NVL-520
Tangpeerachaikul, A., Gu, F., & Pelish, H. E. (2024) · Cancer Research · doi:10.1158/1538-7445.am2024-lb182 · Cited by 1 · see citing works
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Abstract P249: Preclinical antitumor activity of NVL-520 in patient-derived models harboring ROS1 fusions, including G2032R solvent front mutation
Deshpande, A., Yoda, S., Tangpeerachaikul, A., Kohl, N. E., Horan, J. C., Hata, A. N., & Pelish, H. E. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-21-p249
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Authors: Drilon, A., Horan, J. C., Tangpeerachaikul, A., Besse, B., Ou, S.-H. I., Gadgeel, S. M., Camidge, D. R., van der Wekken, A. J., Nguyen-Phuong, L., Acker, A., Keddy, C., Nicholson, K. S., Yoda, S., Mente, S., Sun, Y., Soglia, J. R., Kohl, N. E., Porter, J. R., Shair, M. D., Zhu, V., Davare, M. A., Hata, A. N., Pelish, H. E., & Lin, J. J.
Affiliations: Memorial Sloan Kettering Cancer Center (US)
Nuvalent, Inc. (United States) (US)
Institut Gustave Roussy (FR)
University of California, Irvine Medical Center (US)
Henry Ford Health (US)
University of Colorado Cancer Center (US)
7University of Groningen, University Medical Centre Groningen, Groningen, the Netherlands.
Massachusetts General Hospital (US)
Oregon Health & Science University (US)
Harvard University (US)
Corresponding author: Pelish, Henry E.
Lin, Jessica J.
ORCID: Drilon, Alexander
Horan, Joshua C.
Tangpeerachaikul, Anupong
Besse, Benjamin
Ou, Sai-Hong Ignatius
Gadgeel, Shirish M.
Camidge, D. Ross
van der Wekken, Anthonie J.
Nguyen-Phuong, Linh
Acker, Adam
Keddy, Clare
Nicholson, Katelyn S.
Yoda, Satoshi
Mente, Scot
Sun, Yuting
Soglia, John R.
Kohl, Nancy E.
Porter, James R.
Shair, Matthew D.
Zhu, Viola
Davare, Monika A.
Hata, Aaron N.
Pelish, Henry E.
Lin, Jessica J.
Venue: Cancer Discovery
Publisher: American Association for Cancer Research (AACR)
Published: 2022-12-13
Volume: 13
Issue: 3
Pages: 598-615
ISSN: 2159-8274 (ISSN-L)
2159-8290
DOI: 10.1158/2159-8290.cd-22-0968
PMC: PMC9975673
OpenAlex: W4311280444
Cited by: 52
References: 69
Citations by year: 2026: 10 · 2025: 18 · 2024: 16 · 2023: 8
FWCI: 6.77
Type: journal article
Language: en
Open access: hybrid
doi.org
Licence: cc-by-nc-nd
creativecommons.org/licenses/by-nc-nd/4.0/ (vor, 78 d)
Locations: Cancer Discovery (publishedVersion, cc-by-nc-nd)
PubMed Central (publishedVersion, cc-by-nc-nd)
PubMed (publishedVersion)
University of Groningen research database (University of Groningen / Centre for Information Technology) (submittedVersion, cc-by-nc-nd)
Funders: National Cancer Institute (R01 CA164273, P30 CA008748)
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Health Sciences › Medicine › Pathology and Forensic Medicine › Cancer Mechanisms and Therapy
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Genomics and Diagnostics
Keywords: ROS1 tyrosine kinase inhibitors, brain penetration, crizotinib resistance, brain metastases, patient-derived xenografts, neurotoxicity
MeSH terms: Aminopyridines, Brain, Carcinoma, Non-Small-Cell Lung, Humans, Lactams, Lung Neoplasms, Mutation, Protein-Tyrosine Kinases, Proto-Oncogene Proteins, Pyrazoles, Lactams, Macrocyclic, Protein Kinase Inhibitors

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NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations

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