Resources
In-the-Know With Verastem Oncology
Access the latest posters, presentations and publications from Verastem Oncology below:
Featured Resources
Low-Grade Serous Ovarian Cancer Mechanism of Disease
Verastem Oncology 2024
Jonathan Pachter, Chief Scientific Officer, Discusses the Unique Properties of RAF/MEK Clamp Avutometinib
Jonathan Pachter, PhD, Chief Scientific Officer
Verastem Oncology 2022
Animation Video Demonstrating How Avutometinib and Novel Combinations Better Control RAS Pathway and Parallel Pathway Signaling
Jonathan Pachter, PhD, Chief Scientific Officer
Verastem Oncology 2021
Avutometinib
Avutometinib + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer (ENGOT-ov60/GOG-3052/RAMP 201): Dose Intensity and Subgroup Analysis
Rachel N. Grisham, Els Van Nieuwenhuysen, Carol Aghajanian, Veronique D’Hondt, Bradley J. Monk, Andrew R. Clamp, Emily N. Prendergast, Ana Oaknin, Kari L. Ring, Silvia Derio, Robert Holloway, Manuel Rodrigues, Hye Sook Chon, Charlie Gourley, Alessandro D. Santin, Premal H. Thaker, Christine Gennigens, Gregg Newman, Erin Salinas, Hagop Youssoufian, Kathleen Moore, Stephanie Lustgarten, David M. O’Malley, Toon Van Gorp, Susana N. Banerjee
SGO Annual Meeting on Women’s Cancer, March 14-17, Seattle, WA
Single Arm Phase II Study of Avutometinib and Defactinib in Advanced or Recurrent Mesonephric or Mesonephric-like (MLA) Gynecologic Cancer: Interim Results
Rachel N. Grisham, Aaron Praiss, Alexia Iasonos, Britta Weigelt, Pier Selenica, Angela Green, Robin Guo, Seth Cohen, Salvador Alonso, Maria Rubinstein, Claire Friedman, Joyce Liu, Jeffrey Girshman, Kara Pierro, Carol Aghajanian
SGO Annual Meeting on Women’s Cancer, March 14-17, 2025, Seattle, WA
Efficacy and Safety of Avutometinib ± Defactinib in Recurrent Low-Grade Serous Ovarian Cancer: Primary Analysis of ENGOT-OV60/GOG-3052/RAMP 201
Susana N. Banerjee, Carol Aghajanian, Els Van Nieuwenhuysen, Alessandro D. Santin, Kari L. Ring, Nicoletta Colombo, Premal H. Thaker, Emily N. Prendergast, Kathleen N. Moore, Hye Sook Chon, Andrew R. Clamp, David M. O’Malley, Bradley J. Monk, Alfonso Cortés Salgado, Michel Fabbro, Elsa Kalbacher, Toon Van Gorp, Stephanie Lustgarten, Hagop Youssoufian, Rachel N. Grisham
IGCS Annual Meeting, October 16-18, 2024, Dublin, Ireland
Avutometinib/Defactinib and Gemcitabine/Nab-Paclitaxel Combination in First-Line Metastatic Pancreatic Ductal Adenocarcinoma: Initial Safety and Efficacy of Phase 1b/2 Study (RAMP 205)
Kian-Huat Lim, Kristen R. Spencer, Rachael A. Safyan, Vincent J. Picozzi, Anna M. Varghese, Despina Siolas, Kimberly Perez, Sheena Clift, Louis J. Denis, Vijeta Bhambhani, Stacey Hill, Jonathan A. Pachter, Philippe Pultar, Manuel Hidalgo
ASCO Annual Meeting May 31- June 4, 2024
The SOS1 Inhibitor MRTX0902 Demonstrates Activity Across Cancer Models with Mutations in Proximal Components of the RAS-MAPK Pathway
Niranjan Sudhakar, Larry Yan, Fadia Qiryaqos, Jade Laguer, David M Briere, Allan Hebbert, Andrew Calinisan1, Silvia Coma, Jonathan Pachter, James G Christensen, Peter Olson, and Shilpi Khare Mirati
AACR Annual Meeting; April 5-10, 2024, San Diego
FAK inhibition combined with the RAF/MEK clamp avutometinib overcomes resistance to BRAF and MEK inhibitors and to immune checkpoint blockade in BRAFV600E mutant cutaneous melanoma
Simone Lubrano, Farhoud Faraji, Daniel Cervantes-Villagrana, Sydney Ramirez, Kuniaki Sato, Adam Officier, Nadia Arang, R., Damiano C. Rigiracciolo, Paola Y. Anguiano Quiroz, Sendi R Adame-Garcia, Antonietta Bacchiocchi, Ruth Halaban, Claudia Martini, Silvia Coma, Sheri Holmen, Jonathan A. Pachter, Andrew E. Aplin, J. Silvio Gutkind
AACR Annual Meeting; April 5-10, 2024, San Diego
Combined inhibition of RAF, MEK, and FAK attenuates melanoma brain metastases and prolongs overall survival in preclinical models
Karly Stanley, Jared Almazan, Tursun Turapov, David A. Kircher, Gennie L. Parkman, MiKaela N. Field, Katie M. Culver, Christopher M. Stehn, Silvia Coma, Jonathan A. Pachter, Howard Colman, and Sheri L. Holmen
AACR Annual Meeting; April 5-10, 2024, San Diego
Stromal reprogramming overcomes resistance to RAS/MEK inhibition to improve pancreas cancer responses to cytotoxic therapy
Xiuting Liu, John M, Baer, Meredith L. Stone, Brett L. Knolhoff, Graham D. Hogg, Faiz Ahmad, Jie Chen, Andrew D. Schmidt, Jeffrey A. Klomp, Heather Coho, Kayjana S. Coho, Silvia Coma, Jonathan A. Pachter, Kirsten L. Bryant, Liang-I Kang, Kian H. Lim, Gregory L. Beatty, David G. DeNardo
AACR Annual Meeting; April 5-10, 2024, San Diego
A Phase 3, Randomized Trial Evaluating Avutometinib Plus Defactinib Compared With Investigator’s Choice of Therapy (ICT) in Patients With Recurrent Low-Grade Serous Ovarian Cancer (LGSOC): GOG-3097/ENGOT-ov81/NCRI/RAMP 301
Rachel N. Grisham, Bradley J. Monk, Els Van Nieuwenhuysen, Kathleen N. Moore, Michel Fabbro, David M. O’Malley, Ana Oaknin, Premal H. Thaker, Amit M. Oza, Nicoletta Colombo, Stephanie Lustgarten, Hagop Youssoufian, Susana N. Banerjee
SGO Annual Meeting on Women’s Cancer March 16-18, 2024, San Diego, CA.
Avutometinib + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer (LGSOC): A Subgroup Analysis of ENGOT-ov60/GOG3052/RAMP 201 Part A
Susana N. Banerjee, Els Van Nieuwenhuysen, Alessandro D. Santin, Kari L. Ring, Nicoletta Colombo, Premal H. Thaker, Emily N.
Prendergast, Andrew R. Clamp, Isabelle Ray-Coquard, Hye Sook Chon, Kathleen N. Moore, Erin A. Salinas, Peter G. Rose, David M.
O’Malley, Ana Oaknin, Bradley J. Monk, Robert W. Holloway, Gregg Newman, John W. Moroney, Toon Van Gorp, Elsa Kalbacher,
Christine Gennigens, Nicholas E. Wojtynek, Stephanie Lustgarten, Rachel N. Grisham
SGO Annual Meeting on Women’s Cancer March 16-18, 2024, San Diego, CA
Preclinical efficacy of RAF/MEK clamp avutometinib in combination with FAK inhibition in low grade serous ovarian cancer
Blair McNamara, Michelle Greenman, Cem Demirkiran, Tobias Max Phillip Hartwich, Stefania
Bellone, Diego Manavella, Levent Mutlu, Margherita Zipponi, Yang Yang-Hartwich, Kevin
Yang, Elena Ratner, Peter E. Schwartz, Silvia Coma, Jonathan Pachter, Alessandro D. Santin
SGO Annual Meeting on Women’s Cancer March 16-18, 2024, San Diego, CA
RAF/MEK Clamp Avutometinib: Rational Combinations with FAK Inhibitor and Other Targeted Therapies
Jon Pachter, PhD, Chief Scientific Officer, Verastem Oncology
5th Annual RAS-Targeted Drug Development Summit September 28, 2023
Rational Combinations of RAF/MEK Clamp Avutometinib; Breakthrough Therapy Designation and Beyond
Louis Denis, MD, Chief Medical Officer, Verastem Oncology
5th Annual RAS-Targeted Drug Development Summit September 27, 2023
RAMP 205: A phase 1b/2a study of gemcitabine, nab-paclitaxel, avutometinib, and defactinib in untreated metastatic pancreatic ductal adenocarcinoma
Kian-Huat Lim, Manuel Hidalgo, Mark H. O’Hara, Kristen R. Spencer, Ignacio Garrido-Laguna, David G. DeNardo, Vijeta Bhambhani, Gloria Patrick, Yaofeng Cheng, Silvia Coma, Jonathan A. Pachter, Louis J. Denis
AACR SPECIAL CONFERENCE IN CANCER RESEARCH: PANCREATIC CANCER September 27, 2023
Efficacy and Safety of Avutometinib + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer Following Prior Systemic Therapy
Authors: Rachel N. Grisham, Carol Aghajanian, Els Van Nieuwenhuysen, Manuel Rodrigues, Kari L. Ring, Alessandro D. Santin, Nicoletta Colombo, Emily N. Prendergast, Premal H. Thaker, Katheen N. Moore, Erin A. Salinas, Isabelle Ray-Coquard, Hye Sook Chon, Peter G. Rose, Ana Oaknin, Andrew R. Clamp, Mitul D. Gandhi, Bradley J. Monk, Robert W. Holloway, Toon Van Gorp, Michel Fabbro, Christine Gennigens, Nicholas E. Wojtynek, Stephanie Lustgarten, Susana N. Banerjee
IGCS 2023 Annual Global Meeting, November 5-7, 2023, Seoul, South Korea
Initial Safety, Pharmacokinetics, and Recommended Phase 2 Dose from RAMP 203: A Phase 1/2 Study of Avutometinib + Sotorasib in KRAS G12C Mutant Non-Small Cell Lung Cancer
Authors: Mark M. Awad, Jerome Goldschmidt, Alexander I. Spira, Rajat Malhotra, Jeffrey T. Yorio, Vijeta Bhambhani, Yaofeng Cheng, Pablo S. Lee, Ramaswamy Govindan
AACR –NCI-EORTC 2023 October 14, 2023 Boston, MA
The RAF/MEK clamp avutometinib as the backbone of therapy for pancreatic cancer: Novel combinations with standard of care chemotherapy, FAK inhibitors, KRAS G12D inhibitors and/or autophagy inhibitors
Silvia Coma, Xiuting Liu, Noah L. Pieper, Wen-Hsuan Chang, Kirsten L Bryant, Channing J Der, David G DeNardo, Jonathan A Pachter
AACR Special Conference in Cancer Research: Pancreatic Cancer; Boston September 27-30, 2023
The RAF/MEK clamp avutometinib induces an immunogenic tumor microenvironment and potentiates the efficacy of anti-PD-1
Authors: Silvia Coma, Miriam Molina-Arcas, Julian Downward, Jonathan A. Pachter
Targeting RAS Symposium; Salamanca September 13-15, 2023
The RAF/MEK clamp avutometinib enhances antitumor efficacy of KRAS G12C and G12D inhibitors through vertical inhibition of RAS, RAF and MEK
Silvia Coma, Monica Musteanu, Cristina Caffarra, Alessia Mira, Enrico Patrucco, Julien Dilly, Andrew J Aguirre, Mariano Barbacid, Chiara Ambrogio & Jonathan A Pachter
AACR Special Conference: Targeting RAS
March 5-8, 2023
RAMP 202: A phase 2 study of avutometinib ± defactinib in patients with advanced KRAS G12V mutant non-small cell lung cancer (NSCLC)
Authors: J. Reuss, S. Gandhi, D. Spigel, P. Janne, F. Gardner, L. Paz-Ares Rodriguez, S. Gadgeel, J. Patel, F. Passiglia, A. Spira, M. Edelman, G. Blumenschein, A. Shergill, T. Burns, V. Bhambhani, G. Patrick, J. Pachter, L. Denis, D. Camidge.
ASCO Annual Meeting June 2-6, 2023
Initial efficacy and safety results from ENGOT-ov60/GOG-3052/RAMP201: A phase 2 study of avutometinib ± defactinib in recurrent low-grade serous ovarian cancer (LGSOC)
Authors: S. Banerjee, K. Ring, E. Van Niewenhuysen, M. Fabbro, C. Aghajanian, A. Oaknin, N. Colombo, A. Santin, A. Clamp, K. Moore, P. Rose, D. O’Malley, H. Sook Chon, E. Salinas, E. Prendergast, S. Lustgarten, M. Rodrigues, C. Gennigens, B. Monk, R. Grisham.
ASCO Annual Meeting June 2-6, 2023
The RAF/MEK Clamp Avutometinib as a Backbone of Therapy for RAS Pathway-Driven Cancers: Tumor/Biomarker-Specific Combination Strategies
Silvia Coma, Deborah K Morrison, Monica Musteanu, Chongkai Wang, Julien Dilly, Xiuting Liu, Udai Banerji, Ardaman Shergill, Andrew Aguirre, David G DeNardo, Mariano Barbacid, Marwan Fakih, Jonathan A Pachter
The Fourth RAS Initiative Symposium; October 17 – 19, 2022
Phase I trial of the RAF/MEK clamp Avutometinib in combination with everolimus
Authors: Minchom AR (1), Sanchez Perez V (1), Morton C (2), Manickavasagar T (1), Nintos G (3), Lai-Kwon JE (1), Guo C (1), Tunariu N (1), Parker T (4), Prout T (4), Parmar M (4), Turner AJ (4), Finneran L (4), Hall E (4), Pachter JA (5),
Denis LJ (5), Spicer JF (3), Banerji U (1)
1. Drug Development Unit, The Institute of Cancer Research/The Royal Marsden Hospital NHS Foundation Trust, UK; 2. Guy’s and St Thomas’ NHS Foundation Trust, London, United Kingdom; 3. King’s College London, London, UK ; 4. The Institute of Cancer Research, Sutton, UK; 5. Verastem Oncology, Needham, MA
ASCO Annual Meeting June 3-7, 2022
The RAF/MEK clamp Avutometinib for treatment of cutaneous melanoma harboring BRAF, NRAS, NF1 or RAF1 (CRAF) alterations
Antonella Bacchiocchi, Kamryn Carter, Silvia Coma, Sanjib Chowdhury, Deborah K Morrison, Mario Sznol, Ruth Halaban, Jonathan A Pachter
AACR Annual Meeting – April 8-13, 2022
The RAF/MEK clamp Avutometinib enhances antitumor efficacy of KRAS G12C inhibitors through vertical inhibition of RAS, RAF and MEK
Silvia Coma, Sanjib Chowdhury, Julien Dilly, Monica Musteanu, Deborah K Morrison, Mariano Barbacid, Andrew J Aguirre & Jonathan A Pachter
AACR Annual Meeting – April 8-13, 2022
Mechanistic evaluation of Avutometinib (RAF/MEK clamp) and defactinib (FAK inhibitor) in low-grade serous ovarian cancer models with correlations to clinical response
Adam Stewart, Sara Diaz-Sanchez, Lisa Pickard, Ekta Paranjape, Victoria Sanchez Perez, Sanjib Chowdhury, Stephanie Lustgarten, Silvia Coma, Jonathan A Pachter, Mark Carey, Gabriel DiMattia, Hannah Badham, Toby Prout, Mona Parmar, Muneeb Mahmud, Christina Yap, Matthew Krebs, Susana Banerjee, Udai Banerji
AACR Annual Meeting – April 8-13, 2022
Avutometinib: a Unique RAF/MEK Clamp for Treatment of KRAS Mutant NSCLC
Silvia Coma, Sanjib Chowdhury, Andrew Koustenis, Udai Banerji, Monica Musteanu, Mariano Barbacid, Deborah Morrison, Jonathan A. Pachter
Precision Lung Cancer Summit, January 26, 2022
Dual RAF/MEK inhibitor Avutometinib for treatment of KRAS mutant NSCLC: Novel combinations targeting G12C or G12V variants
Silvia Coma, Sanjib Chowdhury, Monica Musteanu, Adam Stewart, Lisa Pickard, Matthew Krebs, Anna Mincho, Udai Banerji, Mariano Barbacid, Jonathan A. Pachter
IASLC 2021 World Conference on Lung Cancer, September 8-14, 2021
Dual RAF/MEK inhibitor Avutometinib as a Backbone of Therapy for RAS Pathway-Driven Cancers
Silvia Coma, Sanjib Chowdhury, Andrew Koustenis, Udai Banerji, Susana Banerjee, Monica Musteanu, Mariano Barbacid, Marwan Fakih, Chongkai Wang, Jonathan Pachter
RAS Pathway-Driven Cancers, September 23, 2021
Dual RAF/MEK inhibitor Avutometinib for treatment of solid tumors with diverse MAPK pathway alterations
Silvia Coma, Sanjib Chowdhury, Monica Musteanu, Mariano Barbacid, Jonathan A. Pachter
AACR-NCR-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics, October 7-10, 2021
Phase I study of the combination of the dual RAF/MEK inhibitor Avutometinib and the FAK inhibitor defactinib: Results of efficacy in low grade serous ovarian cancer
S. Banerjee, R. Grochot, R. Shinde, J. Lima, M. Krebs, R. Rahman, M. Little, N. Tunariu, A. Curcean, H. Badham, M. Mahmud, A. Turner, M. Parmar, C. Yap, A. Minchom, J.
Lopez, J. de Bono, U. Banerji.
2021 ESMO Congress
Clinical Combinations: Dual RAF-MEK & FAK Inhibition for the Treatment of KRAS Mutant Cancers With a Focus on Low-Grade Serous Ovarian Cancer
Dr. Udai Banerji
RAS-Targeted Drug Development – September 16, 2020
CRAF, but Not BRAF, Is Essential for Development of KRAS Oncogene-Driven Non-Small Cell Lung Carcinoma
Rafael B. Blasco, Sarah Francoz, David SantamarÃa, Marta Cañamero, Pierre Dubus, Jean Charron, Manuela Baccarini, and Mariano Barbacid
Cancer Cell. 2011 May 17; 19(5): 652–663. doi:10.1016/j.ccr.2011.04.002
First-in-Human, Phase I Dose-Escalation Study of the Safety, Pharmacokinetics, and Pharmacodynamics of RO5126766, a First-in-Class Dual RAF/MEK Inhibitor in Patients With Solid Tumors
Maria Martinez-Garcia, Udai Banerji, Joan Albanell, Rastilav Bahleda, Saoirse Dolly, Françoise Kraeber-Bodéré, Federico Rojo, Emilie Routier, Ernesto Guarin, Zhi-Xin Xu, Ruediger Rueger, Jean J. L. Tessier, Eliezer Shochat, Steve Blotner, Valerie Meresse Naegelen and Jean-Charles Soria
Clin Cancer Res. 2012 September 1; (18) (17): 4806-4819. doi: 10.1158/1078-0432.CCR-12-0742
Enhanced Inhibition of ERK Signaling by a Novel Allosteric MEK Inhibitor, CH5126766 (avutometinib), That Suppresses Feedback Reactivation of RAF Activity
Nobuya Ishii, Naoki Harada, Eric W. Joseph, Kazuhiro Ohara, Takaaki Miura, Hiroshi Sakamoto, Yutaka Matsuda, Yasushi Tomii, Yukako Tachibana-Kondo, Hitoshi Iikura, Toshihiro Aoki, Nobuo Shimma, Mikio Arisawa, Yoshihiro Sowa, Poulikos I. Poulikakos, Neal Rosen, Yuko Aoki, and Toshiyuki Sakai
Cancer Res. 2013 July 1; 73(13): 4050–4060. doi:10.1158/0008-5472.CAN-12-3937
Disruption of CRAF-Mediated MEK Activation Is Required for Effective MEK Inhibition in KRAS Mutant Tumors
Piro Lito, Anna Saborowski, Jingyin Yue, Martha Solomon, Eric Joseph, Sunyana Gadal, Michael Saborowski, Edward Kastenhuber, Christof Fellmann, Kazuhiro Ohara, Kenji Morikami, Takaaki Miura, Christine Lukacs, Nobuya Ishii, Scott Lowe, and Neal Rosen
Cancer Cell. 2014 May 12; 25(5): 697–710. doi:10.1016/j.ccr.2014.03.011
Phase I Study of the Combination of a RAF/MEK Inhibitor CH5126766 and FAK Inhibitor Defactinib in an Intermittent Dosing Schedule With Expansions in KRAS Mutant Cancers
Rajiv Shinde, Angelika Terbuch, Martin Little, Reece Caldwell, Roopa Kurup, Ruth Riisnaes, Mateus Crespo, Ruth Ruddle, Bora Gurel, Adam Stewart, Jenny King, Mona Parmar, Alison Turner, Florence Raynaud, Muneeb Mahmud, Christina Yap, Jonathan A. Pachter, Gordon B. Mills, Anna Minchom, Juanita Lopez, Susana N. Banerjee, Johann S. de Bono, Matthew Krebs, Udai Banerji
AACR Session I April 24-29, 2020 & Session II June 22-24, 2020
Synergistic Combinations With the Dual RAF/MEK Inhibitor Avutometinib to Overcome Resistance Mechanisms
Jonathan Pachter, PhD
RAS-Targeted Drug Development – September 16, 2020
Intermittent Schedules of the Oral RAF/MEK Inhibitor CH5126766/Avutometinib in Patients With RAS/RAF-Mutant Solid Tumours and Multiple Myeloma: a Single-Centre, Open-Label, Phase 1 Dose-Escalation and Basket Dose-Expansion Study
Christina Guo, Maxime Chénard-Poirier, Desamparados Roda, Maria de Miguel, Samuel J Harris, Irene Moreno Candilejo, Priya Sriskandarajah, Wen Xu, Mariana Scaranti, Anastasia Constantinidou, Jenny King, Mona Parmar, Alison J Turner, Suzanne Carreira, Ruth Riisnaes, Laura Finneran, Emma Hall, Yuji Ishikawa, Kiyohiko Nakai, Nina Tunariu, Bristi Basu, Martin Kaiser, Juanita Suzanne Lopez, Anna Minchom, Johann S de Bono, Udai Banerji
Lancet Oncology. 2020 October 28; 21 (11): 1478-1488. DOI: 10.1016/S1470-2045(20)30464-2
Synthetic Lethal Screens Reveal Co-Targeting FAK and MEK as a Multimodal Precision Therapy for GNAQ-Driven Uveal Melanoma
Justine S. Paradis, Monica Acosta, Robert Saddawi-Konefka, Ayush Kishore, Frederico Gomes, Nadia Arang, Manoela Tiago, Silvia Coma, Simone Lubrano, Xingyu Wu, Kyle Ford, Chi-Ping Day, Glenn Merlino, Prashant Mali, Jonathan A. Pachter, Takami Sato, Andrew E. Aplin, J. Silvio Gutkind
Clinical Cancer Research. 2021 February 10; DOI: 10.1158/1078-0432.CCR-20-3363
Synergistic Combinations With the Novel Dual RAF/MEK Inhibitor: Establishing Avutometinib as the Backbone of Therapy for RAS-Driven Cancers
Silvia Coma, Sanjib Chowdhury, Jonathan A. Pachter
RAS-Targeted Drug Discovery Summit – February 23-25, 2021
Synergistic Antitumor Efficacy of the Dual RAF/MEK Inhibitor Avutometinib With FAK Inhibition for Treatment of RAS-Dependent Solid Tumors
Silvia Coma, Monica Musteanu, Justine S. Paradis, J. Silvio Gutkind, Mariano Barbacid, Jonathan A. Pachter
AACR Virtual Annual Meeting – April 10-15, 2021 & May 17-21, 2021
Dual RAF/MEK Inhibitor Avutometinib Enhances Anti-Tumor Efficacy of KRAS G12C Inhibitors Through a Vertical Pathway Inhibition Strategy
Silvia Coma, Sanjib Chowdhury, Jonathan A Pachter
AACR Virtual Annual Meeting – April 10-15, 2021 & May 17-21, 2021
FRAME: A Phase I Trial of the Combination of the Dual RAF/MEK Inhibitor Avutometinib and the FAK Inhibitor Defactinib; Evaluation of Efficacy in KRAS Mutated NSCLC
Matthew G. Krebs, Rajiv Shinde, Rozana Abdul Rahman, Rafael Grochot, Martin Little, Jenny King, Mark Van De Velde, Joseph Kitchin, Mona Parmar, Alison Turner, Muneeb Mahmud, Christina Yap, Nina Tunariu, Juanita Lopez, Johann S. de Bono, Udai Banerji, Anna Minchom
AACR Virtual Annual Meeting – April 10-15, 2021 & May 17-21, 2021
Searching for Treatments for Non-G12C-KRAS Mutant Cancers
Christina Guo & Udai Banerji
British Journal of Cancer (2021) – April 15, 2021
Dual RAF/MEK Inhibitor Avutometinib for Treatment of KRAS Mutant NSCLC: Novel Combinations Targeting G12V or G12C Variants
Jonathan Pachter, PhD, Chief Scientific Officer
NSCLC Drug Development Summit – July 14, 2021
Defactinib
A Phase I Study of VS-6063, a Second-Generation Focal Adhesion Kinase Inhibitor, in Patients With Advanced Solid Tumors
Suzanne F Jones, Lillian L Siu, Johanna C Bendell, James M Cleary, Albiruni R A Razak, Jeffrey R Infante, Shuchi S Pandya, Philippe L Bedard, Kristen J Pierce, Brett Houk, W Gregory Roberts, S Martin Shreeve, Geoffrey I Shapiro
Invest New Drugs. 2015 Oct;33(5):1100-7. doi: 10.1007/s10637-015-0282-y
Targeting Focal Adhesion Kinase Renders Pancreatic Cancers Responsive to Checkpoint Immunotherapy
Hong Jiang, Samarth Hegde, Brett L. Knolhoff, Yu Zhu1, John M. Herndon, Melissa A. Meyer, Timothy M. Nywening, William G. Hawkins, Irina M. Shapiro, David T. Weaver, Jonathan A. Pachter, Andrea Wang-Gillam, and David G. DeNardo
Nat Med. 2016 August; 22(8): 851–860. doi:10.1038/nm.4123
Nuclear FAK Controls Chemokine Transcription, Tregs, and Evasion of Anti-tumor Immunity
Alan Serrels, Tom Lund, Bryan Serrels, Adam Byron, Rhoanne C. McPherson, Alexander von Kriegsheim, Laura Go´ mez-Cuadrado, Marta Canel, Morwenna Muir, Jennifer E. Ring, Eleni Maniati, Andrew H. Sims, Jonathan A. Pachter, Valerie G. Brunton, Nick Gilbert, Stephen M. Anderton, Robert J.B. Nibbs, and Margaret C. Frame
Cell. 2016 September 24; 163(1): 160-173. doi: 10.1016/j.cell.2015.09.001
FAK Activity Sustains Intrinsic and Acquired Ovarian Cancer Resistance to Platinum Chemotherapy
Carlos J Diaz Osterman, Duygu Ozmadenci, Elizabeth G Kleinschmidt, Kristin N Taylor, Allison M Barrie, Shulin Jiang, Lisa M Bean, Florian J Sulzmaier, Christine Jean, Isabelle Tancioni, Kristen Anderson, Sean Uryu, Edward A Cordasco, Jian Li, Xiao Lei Chen, Guo Fu, Marjaana Ojalill, Pekka Rappu, Jyrki Heino, Adam M Mark, Guorong Xu, Kathleen M Fisch, Vihren N Kolev, David T Weaver, Jonathan A Pachter, Balázs Győrffy, Michael T McHale, Denise C Connolly, Alfredo Molinolo, Dwayne G Stupack, and David D Schlaepfer
eLife. 2019; 8: e47327. Published online 2019 Sep 3. doi: 10.7554/eLife.47327
Phase 2 Study of the Focal Adhesion Kinase Inhibitor Defactinib (VS-6063) in Previously Treated Advanced KRAS Mutant Non-Small Cell Lung Cancer
David E. Gerber, D. Ross Camidge, Daniel Morgensztern, Jeremey Cetnar, Ronan J. Kelly, Suresh S. Ramalingam, David R. Spigel, Woondong Jeong, Pier P. Scaglioni, Song Zhang, Marilyn Li, David T. Weaver, Louis Vaikus, Mitchell Keegan, Joanna C. Horobin, and Timothy F. Burns
Lung Cancer. 2020 Jan; 139: 60–67. doi: 10.1016/j.lungcan.2019.10.033
Phase I Study of Defactinib Combined With Pembrolizumab and Gemcitabine in Patients With Advanced Cancer: Experiences of Pancreatic Ductal Adenocarcinoma (PDAC) Patients
Andrea Wang-Gillam, Robert McWilliams, A. Craig Lockhart, Benjamin R. Tan Jr., Rama Suresh, Kian-Huat Lim, Katrina S. Pedersen, Nikolaos Trikalinos, Olivia Aranha, Haeseong Park, Lee Ratner, Nicholas Boice, David G DeNardo.
AACR Session I April 24-29, 2020 & Session II June 22-24, 2020
Targeting FAK in Anticancer Combination Therapies
John C. Dawson, Alan Serrels, Dwayne G. Stupack, David D. Schlaepfer & Margaret C. Frame
Nature Reviews Cancer. 2021 March 17; doi.org/10.1038/s41568-021-00340-6
GFH375 (VS-7375) KRAS G12D (ON/OFF) Inhibitor
GFH375 (VS-7375): An oral, selective KRAS G12D (ON/OFF) inhibitor with potent anti-tumor efficacy
Feng Yan, Tao Jiang, Tao Liang, Lijian Cai, Leitao Zhang, Xiaoming Xu, Yanhui Zhao, Xiaoling Lan, Xiaohui Zhang, Meng Liu, Qiang Liu, Jinting Gao, Fubo Xie, Xueyan Gao, Li Wang, Jingyang Zhang, Hongcan Ren, Dong Liu, Siyuan Le, Lili Tang, Silvia Coma, Yaofeng Cheng, Nathan Sanburn, Jonathan A. Pachter, Fusheng Zhou, Jiong Lan, Qiang Lu, Genfleet Therapeutics, Shanghai, China, Verastem Oncology, Needham, MA
AACR Annual Meeting; San Diego April 5-10