The scientific foundations of OPC080 are the result of several years of collaborative research in medicinal chemistry, kinase biology, computational drug design, and pancreatic cancer.
The publications below describe the key discoveries and technological advances that ultimately led to the identification and optimization of OPC080 as a novel therapeutic candidate.
A comprehensive peer-reviewed manuscript reporting the complete preclinical characterization of OPC080 is currently under submission and will be referenced here once published.

(1) Mont, N.; Teixido, J.; Borrell, J. I. A diversity oriented, microwave assisted synthesis of N-substituted 2-hydro-4-amino-pyrido 2,3-d pyrimidin-7(8H)-ones. Molecular Diversity 2009, 13 (1), 39-45. DOI: 10.1007/s11030-008-9096-6.

(2) Berzosa, X.; Bellatriu, X.; Teixido, J.; Borrell, J. I. An Unusual Michael Addition of 3,3-Dimethoxypropanenitrile to 2-Aryl Acrylates: A Convenient Route to 4-Unsubstituted 5,6-Dihydropyrido 2,3-d pyrimidines. Journal of Organic Chemistry 2010, 75 (2), 487-490. DOI: 10.1021/jo902345r.

(3) Galve, I.; de la Bellacasa, R. P.; Sanchez-Garcia, D.; Batllori, X.; Teixido, J.; Borrell, J. I. Synthesis of 2-arylamino substituted 5,6-dihydropyrido 2,3-d pyrimidine-7(8H)-ones from arylguanidines. Molecular Diversity 2012, 16 (4), 639-649. DOI: 10.1007/s11030-012-9398-6.

(4) Camarasa, M.; Barnils, C.; de la Bellacasa, R. P.; Teixido, J.; Borrell, J. I. A new and practical method for the synthesis of 6-aryl-5,6-dihydropyrido 2,3- pyrimidine-4,7(3,8)-diones. Molecular Diversity 2013, 17 (3), 525-536. DOI: 10.1007/s11030-013-9450-1.

(5) de la Bellacasa, R. P.; Roue, G.; Balsas, P.; Perez-Galan, P.; Teixido, J.; Colomer, D.; Borrell, J. I. 4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido 2,3-d pyrimidin-7-(8H) -ones as BCR kinase inhibitors for B lymphoid malignancies. European Journal of Medicinal Chemistry 2014, 86, 664-675. DOI: 10.1016/j.ejmech.2014.09.018.

(6) Silvia, G.; Molina-Vila, M. A.; Borrell, J. I.; de la Bellacasa, R. P.; Morales, D.; Bertran-Alamillo, J.; Gimenez-Capitan, A.; Karachaliou, N.; Rosell, R. PB1 a new DDR2 inhibitor: Potential treatment to SCC patients. European Journal of Cancer 2015, 51, S642-S642. DOI: 10.1016/s0959-8049(16)31759-2.

(7) Camarasa, M.; de la Bellacasa, R. P.; Gonzalez, A. L.; Ondono, R.; Estrada, R.; Franco, S.; Badia, R.; Este, J.; Martinez, M. A.; Teixido, J.; et al. Design, synthesis and biological evaluation of pyrido 2,3-d pyrimidin-7-(8H)-ones as HCV inhibitors. European Journal of Medicinal Chemistry 2016, 115, 463-483. DOI: 10.1016/j.ejmech.2016.03.055.

(8) Garcia-Roman, S.; Molina, M. A.; Borrell, J. I.; de la Bellacasa, R. P.; Morales, D.; Bertran, J.; Gimenez, A.; Karachaliou, N.; Rosell, R. PB1, a DDR2 inhibitor with antitumor activity in preclinical models of squamous cell carcinoma and KRAS-mutated adenocarcinoma of the lung. Cancer Research 2016, 76. DOI: 10.1158/1538-7445.am2016-4802.

(9) Galve, I.; Ondono, R.; de Rocafiguera, C.; de la Bellacasa, R. P.; Batllori, X.; Puigjaner, C.; Font-Bardia, M.; Vallcorba, O.; Teixido, J.; Borrell, J. I. A captured room temperature stable Wheland intermediate as a key structure for the orthogonal decoration of 4-amino-pyrido 2,3-d pyrimidin-7(8H)-ones. Organic & Biomolecular Chemistry 2020, 18 (48). DOI: 10.1039/d0ob01785j.

(10) de Rocafiguera, C.; Lloveras, V.; Vidal-Gancedo, J.; Teixidó, J.; Estrada-Tejedor, R.; Borrell, J. I.; de la Bellacasa, R. P. Autocatalytic photoinduced oxidative dehydrogenation of pyrido 2,3-<i>d</i> pyrimidin-7(8<i>H</i>)-ones: synthesis of C5-C6 unsaturated systems with concomitant formation of a long-lived radical. Organic Chemistry Frontiers 2023, 11 (1), 27-36. DOI: 10.1039/d3qo01358h.

(11) Dulsat, J.; Lopez-Nieto, B.; Estrada-Tejedor, R.; Borrell, J. I. Evaluation of Free Online ADMET Tools for Academic or Small Biotech Environments. Molecules 2023, 28 (2). DOI: 10.3390/molecules28020776.

(12) Dulsat, J.; de la Bellacasa, R.; Borrell, J. The Use of a Penta-Deuterophenyl Substituent to Improve the Metabolic Stability of a Tyrosine Kinase Inhibitor. Molecules 2024, 29 (24). DOI: 10.3390/molecules29246042.

(13) Torres-Urtizberea, E.; Borrell, J.; de la Bellacasa, R.; Estrada-Tejedor, R. Rational Method for Structural Simplification as Key Step in Hit Discovery: The Case of FGFR2 and IGF1R Dual Inhibitors. International Journal of Molecular Sciences 2025, 26 (9). DOI: 10.3390/ijms26094457.