The discovery and evaluation of [18F]BMS-986229, a novel macrocyclic peptide PET radioligand for the measurement of PD-L1 expression and in-vivo PD-L1 target engagement

Yu Xin J, Hubbard-Lucey VM, Tang J. Immuno-oncology drug development goes global. Nat Rev Drug Discov. 2019;18:899–900.

Article  Google Scholar 

Forde PM, Spicer J, Lu S, Provencio M, Mitsudomi T, Awad MM, Felip E, Broderick SR, Brahmer JR, Swanson SJ, Kerr K, Wang C, Ciuleanu T-E, Saylors GB, Tanaka F, Ito H, Chen K-N, Liberman M, Vokes EE, Taube JM, Dorange C, Cai J, Fiore J, Jarkowski A, Balli D, Sausen M, Pandya D, Calvet CY, Girard N. Neoadjuvant Nivolumab plus chemotherapy in resectable lung cancer. N Engl J Med. 2022;386(21):1973–85.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Riella LV, Paterson AM, Sharpe AH, Chandraker A. Role of the PD-1 pathway in the immune response. Am J Transplant. 2012;12:2575–87.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Keir ME, Butte MJ, Freeman GJ, Sharpe AH. PD-1 and its ligands in tolerance and immunity. Annu Rev Immunol. 2008;26:677–704.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Freeman GJ, Long AJ, Iwai Y, Bourque K, Chernova T, Nishimura H, Fitz LJ, Malenkovich N, Okazaki T, Byrne MC, Horton HF, Fouser L, Carter L, Ling V, Bowman MR, Carreno BM, Collins M, Wood CR, Honjo T. Engagement of the PD-1 immunoinhibitory receptor by a novel B7 family member leads to negative regulation of lymphocyte activation. J Exp Med. 2000;192:1027–34.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Herbst RS, Soria J-C, Kowanetz M, Fine GD, Hamid O, Gordon MS, Sosman JA, McDermott DF, Powderly JD, Gettinger SN, Kohrt HEK, Horn L, Lawrence DP, Rost S, Leabman M, Xiao Y, Mokatrin A, Koeppen H, Hegde PS, Mellman I, Chen DS, Hodi FS. Predictive correlates of response to the anti-PD-L1 antibody MPDL3280A in cancer patients. Nature (London, U K). 2014;515:563–7.

Article  CAS  Google Scholar 

Rittmeyer A, Barlesi F, Waterkamp D, Ballinger M, Kowanetz M, He P, Chen DS, Sandler A, Park K, Ciardiello F, von Pawel J, Gadgeel SM, Hida T, Kowalski DM, Dols MC, Cortinovis DL, Leach J, Polikoff J, Barrios C, Kabbinavar F, Frontera OA, De MF, Turna H, Lee J-S, Gandara DR. Atezolizumab versus docetaxel in patients with previously treated non-small-cell lung cancer (OAK): a phase 3, open-label, multicentre randomised controlled trial. Lancet. 2017;389:255–65.

Article  PubMed  Google Scholar 

Antonia SJ, Villegas A, Daniel D, Vicente D, Murakami S, Hui R, Yokoi T, Chiappori A, Lee KH, de Wit M, Cho BC, Bourhaba M, Quantin X, Tokito T, Mekhail T, Planchard D, Kim Y-C, Karapetis CS, Hiret S, Ostoros G, Kubota K, Gray JE, Paz-Ares L, de Castro Carpeño J, Wadsworth C, Melillo G, Jiang H, Huang Y, Dennis PA, Ozguroglu M. Durvalumab after chemoradiotherapy in stage III non-small-cell lung cancer. N Engl J Med. 2017;377:1919–29.

Article  PubMed  CAS  Google Scholar 

Le DT, Uram JN, Wang H, Bartlett BR, Kemberling H, Eyring AD, Skora AD, Luber BS, Azad NS, Laheru D, Biedrzycki B, Donehower RC, Zaheer A, Fisher GA, Crocenzi TS, Lee JJ, Duffy SM, Goldberg RM, de la Chapelle A, Koshiji M, Bhaijee F, Huebner T, Hruban RH, Wood LD, Cuka N, Pardoll DM, Papadopoulos N, Kinzler KW, Zhou S, Cornish TC, Taube JM, Anders RA, Eshleman JR, Vogelstein B, Diaz LA Jr. PD-1 blockade in tumors with mismatch-repair deficiency. N Engl J Med. 2015;372:2509–20.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Kazandjian D, Suzman DL, Blumenthal G, Mushti S, He K, Libeg M, Keegan P, Pazdur R. FDA approval summary: nivolumab for the treatment of metastatic non-small cell lung cancer with progression on or after platinum-based chemotherapy. Oncologist. 2016;21:634–42.

Article  PubMed  PubMed Central  CAS  Google Scholar 

He J, Hu Y, Hu M, Li B. Development of PD-1/PD-L1 Pathway in Tumor Immune Microenvironment and Treatment for Non-Small Cell Lung Cancer. Sci Rep. 2015;5:13110.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Shukuya T, Carbone DP. Predictive Markers for the Efficacy of Anti-PD-1/PD-L1 Antibodies in Lung Cancer. J Thorac Oncol. 2016;11:976–88.

Article  PubMed  PubMed Central  Google Scholar 

Robu S, Richter A, Seidl C, Weber WA, Gosmann D, Aulehner C, Krackhardt AM, Leung D, Hayes W, Cohen D, Morin P, Donnelly DJ, Lipovsek D, Bonacorsi SJ, Smith A, Steiger K, Steiger K, Krackhardt AM, Weber WA, Weber WA. Synthesis and preclinical evaluation of a [68Ga]-labeled adnectin, [68Ga]-BMS-986192, as a PET agent for imaging PD-L1 expression. J Nucl Med. 2021;62:1228–34.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Donnelly DJ, Smith RA, Morin P, Lipovsek D, Gokemeijer J, Cohen D, Lafont V, Tran T, Cole EL, Wright M, Kim J, Pena A, Kukral D, Dischino DD, Chow P, Gan J, Adelakun O, Wang XT, Cao K, Leung D, Bonacorsi SJ Jr, Hayes W. Synthesis and biologic evaluation of a novel 18F-labeled adnectin as a PET radioligand for imaging PD-L1 expression. J Nucl Med. 2018;59:529–35.

Article  PubMed  CAS  Google Scholar 

Niemeijer AN, Leung D, Huisman MC, Bahce I, Hoekstra OS, van Dongen GAMS, Boellaard R, Du S, Hayes W, Smith R, Windhorst AD, Hendrikse NH, Poot A, Vugts DJ, Thunnissen E, Morin P, Lipovsek D, Donnelly DJ, Bonacorsi SJ, Velasquez LM, de Gruijl TD, Smit EF, de Langen AJ. Whole body PD-1 and PD-L1 positron emission tomography in patients with non-small-cell lung cancer. Nat Commun. 2018;9:1–5.

Article  CAS  Google Scholar 

Stutvoet TS, van der Veen EL, Kol A, Antunes IF, de Vries EFJ, Hospers GAP, de Vries EGE, de Jong S, Lub-de Hooge MN. Molecular imaging of PD-L1 expression and dynamics with the adnectin-based PET tracer 18F-BMS-986192. J Nucl Med. 2020;61:1839–45.

Article  PubMed  CAS  Google Scholar 

Zhou H, Bao G, Wang Z, Zhang B, Li D, Chen L, Deng X, Yu B, Zhao J, Zhu X, Zhao J, Zhao J. PET imaging of an optimized anti-PD-L1 probe [68Ga]-NODAGA-BMS-986192 in immunocompetent mice and non-human primates. EJNMMI Res. 2022;12:35.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Nienhuis PH, Antunes IF, Glaudemans AWJM, Noordzij W, Slart RHJA, de Vries EFJ, Jalving M, Hospers GAP, Leung D, Slart RHJA. 18F-BMS-986192 PET imaging of PD-L1 in metastatic melanoma patients with brain metastases treated with immune checkpoint inhibitors: a pilot study. J Nucl Med. 2022;63:899–905.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Donnelly David J. PET imaging in drug discovery and development. In: Handbook of Radiopharmaceuticals, 2nd edn. 2020;703–725. https://doi.org/10.1002/9781119500575.ch22.

Scola P, et al. Discovery of BMS-986189, a Macrocyclic Peptide Inhibitor of PD-L1, manuscript submitted to ACS Med. Chem Lett. 2023.

Cole EL, Kim J, Donnelly DJ, Smith RA, Cohen D, Lafont V, Morin PE, Huang RYC, Chow PL, Hayes W, Bonacorsi S Jr. Radiosynthesis and preclinical PET evaluation of 89Zr-nivolumab (BMS-936558) in healthy non-human primates. Bioorg Med Chem. 2017;25:5407–14.

Article  PubMed  CAS  Google Scholar 

Wei W, Zhang D, Wang C, Zhang Y, An S, Chen Y, Huang G, Liu J. Annotating cd38 expression in multiple myeloma with [18F]F-Nb1053. Mol Pharm. 2022;19(10):3502–10.

Article  PubMed  CAS  Google Scholar 

Kumar D, Lisok A, Dahmane E, McCoy M, Shelake S, Chatterjee S, Allaj V, Sysa-Shah P, Wharram B, Lesniak WG, Tully E, Gabrielson E, Jaffee EM, Poirier JT, Rudin CM, Gobburu JV, Pomper MG, Nimmagadda S. Peptide-based PET quantifies target engagement of PD-L1 therapeutics. J Clin Invest. 2019;129:616–30.

Article  PubMed  PubMed Central  Google Scholar 

Lesniak WG, Mease RC, Chatterjee S, Kumar D, Lisok A, Wharram B, Kalagadda VR, Emens LA, Pomper MG, Nimmagadda S. Development of [18F]FPy-WL12 as a PD-L1 specific PET imaging peptide. Mol Imaging. 2019;18:1–9.

Article  CAS  Google Scholar 

Jouini N, Cardinale J, Mindt TL, Jouini N, Mindt TL, Jouini N, Cardinale J, Mindt TL. Evaluation of a radiolabeled macrocyclic peptide as potential PET imaging probe for PD-L1. ChemMedChem. 2022;17: e202200091.

Article  PubMed  PubMed Central  CAS  Google Scholar 

De Silva RA, Kumar D, Lisok A, Chatterjee S, Wharram B, Venkateswara Rao K, Mease R, Dannals RF, Pomper MG, Nimmagadda S. Peptide-based 68Ga-PET radiotracer for imaging PD-L1 expression in cancer. Mol Pharm. 2018;15:3946–52.

Article  PubMed  PubMed Central  Google Scholar 

Lin D, Wallace M, Allentoff AJ, Donnelly DJ, Gomes E, Voronin K, Gong S, Huang RYC, Kim H, Caceres-Cortes J, Bonacorsi S. Chemoselective methionine bioconjugation: Site-selective fluorine-18 labeling of proteins and peptides. Bioconjug Chem. 2020;31:1908–16.

Article  PubMed  CAS  Google Scholar 

Donnelly D. Methods and compositions for 18F-radiolabeling of biologics. Methods and compositions for 18f-radiolabeling of biologics - Google Patents. Princeton , NJ: BRISTOL -M YERS SQUIBB Publication Classification Company. 2022.

Donnelly D, Leung DK. Imaging methods using 18F-radiolabeled biologics. Imaging methods using 18f-radiolabeled biologics - Google Patents. Princeton , NJ: BRISTOL -M YERS SQUIBB Publication Classification Company. 2021. 

Brahmer JR, Tykodi SS, Chow LQM, Hwu W-J, Topalian SL, Hwu P, Drake CG, Camacho LH, Kauh J, Odunsi K, Pitot HC, Hamid O, Bhatia S, Martins R, Eaton K, Chen S, Salay TM, Alaparthy S, Grosso JF, Korman AJ, Parker SM, Agrawal S, Goldberg SM, Pardoll DM, Gupta A, Wigginton JM. Safety and activity of Anti–PD-L1 antibody in patients with advanced cancer. N Engl J Med. 2012;366:2455–65.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Hotchkiss RS, Colston E, Yende S, Angus DC, Moldawer LL, Crouser ED, Martin GS, Coopersmith CM, Brakenridge S, Mayr FB, Park PK, Ye J, Catlett IM, Girgis IG, Grasela DM. Immune checkpoint inhibition in sepsis: a phase 1b randomized, placebo-controlled, single ascending dose study of antiprogrammed cell death-ligand 1 antibody (BMS-936559). Crit Care Med. 2019;47:632–42.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Gay CL, Bosch RJ, Ritz J, Hataye JM, Aga E, Tressler RL, Mason SW, Hwang CK, Grasela DM, Ray N, Cyktor JC, Coffin JM, Acosta EP, Koup RA, Mellors JW, Eron JJ. Clinical trial of the anti-PD-L1 antibody BMS-936559 in HIV-1 infected participants on suppressive antiretroviral therapy. J Infect Dis. 2017;215:1725–33.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Postow MA, Mauguen A, Frosina D, et al. Assessing PD-L1 without a biopsy and through PD-L1 PET imaging with [18F]BMS-986229. J Clin Oncol. 2022;40(11):Supplement. Abstract #2578.

Cytryn S, Lumish M, Paroder V, et al. Feasibility, safety, and biodistribution of [18F]BMS-986229 PET in patients with esophagogastric (EG) cancer. Ann Oncol. 2022;33(Suppl_4):S335, P-244.

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