Results 11 to 20 of about 1,458 (171)

Solubility Modeling for Key Organic Compounds Used in Adavosertib (Anticancer API) Manufacturing. [PDF]

ACS Omega
The solubility of organic compounds plays an important role in pharmaceutical manufacturing since key unit operations such as reactors, crystallizers, and solvent extraction units all rely on successful reagent and product dissolution. Consequently, predictive solubility modeling is very useful when developing new pharmaceutical processes, so as to ...
Blair M, Chalchooghi MM, Cox RJ, Gerogiorgis DI.   +3 more
europepmc   +7 more sources

Targeted inhibition of the methyltransferase SETD8 synergizes with the Wee1 inhibitor adavosertib in restraining glioblastoma growth

Cell Death and Disease, 2023
Despite intense research efforts, glioblastoma remains an incurable brain tumor with a dismal median survival time of 15 months. Thus, identifying new therapeutic targets is an urgent need.
Rosa Della Monica, Michela Buonaiuto, Mariella Cuomo, Cristina Pagano, Federica Trio, Davide Costabile, Giulia de Riso, Francesca Sveva Cicala, Maddalena Raia, Raduan Ahmed Franca, Marialaura Del Basso De Caro, Domenico Sorrentino, Giovanna Navarra, Laura Coppola, Lorella Tripodi, Lucio Pastore, Juergen Hench, Stephan Frank, Claudio Schonauer, Giuseppe Catapano, Maurizio Bifulco, Lorenzo Chiariotti, Roberta Visconti   +22 more
doaj   +5 more sources

Adavosertib Enhances Antitumor Activity of Trastuzumab Deruxtecan in HER2-Expressing Cancers [PDF]

Clinical Cancer Research, 2023
Abstract Purpose: Cyclin E (CCNE1) has been proposed as a biomarker of sensitivity to adavosertib, a Wee1 kinase inhibitor, and a mechanism of resistance to HER2-targeted therapy. Experimental Design: Copy number and ...
Timothy P. DiPeri, Kurt W. Evans, Maria Gabriela Raso, Ming Zhao, Yasmeen Q. Rizvi, Xiaofeng Zheng, Bailiang Wang, Bryce P. Kirby, Kathleen Kong, Michael Kahle, Timothy A. Yap, Ecaterina E. Dumbrava, Jaffer A. Ajani, Siqing Fu, Khandan Keyomarsi, Funda Meric-Bernstam   +15 more
openaire   +3 more sources

WEE1 inhibitor adavosertib in combination with carboplatin in advanced TP53 mutated ovarian cancer: A biomarker-enriched phase II study [PDF]

Gynecologic Oncology, 2023
In the first part of this phase II study (NCT01164995), the combination of carboplatin and adavosertib (AZD1775) was shown to be safe and effective in patients with TP53 mutated platinum-resistant ovarian cancer (PROC). Here, we present the results of an additional safety and efficacy cohort and explore predictive biomarkers for resistance and response
Embaby, Alaa, Kutzera, Joachim, Geenen, Jill J, Pluim, Dick, Hofland, Ingrid, Sanders, Joyce, Lopez-Yurda, Marta, Beijnen, Jos H, Huitema, Alwin D R, Witteveen, Petronella O, Steeghs, Neeltje, van Haaften, Gijs, van Vugt, Marcel A T M, de Ridder, Jeroen, Opdam, Frans L   +14 more
core   +5 more sources

Synergistic interactions of cytarabine-adavosertib in leukemic cell lines proliferation and metabolomic endpoints

Biomedicine & Pharmacotherapy, 2023
Drug synergy allows reduced dosing, side effects and tolerance. Optimization of drug synergy chemotherapy is fundamental in acute lymphocytic leukemia and other cancers. This study aimed to analyze the pharmacodynamic synergy between the anti-metabolite cytarabine and WEE1 inhibitor adavosertib on acute leukemia cell lines CCRF-CEM and Jurkat.
Gabriel O. Rodríguez-Vázquez, Adriana O. Diaz-Quiñones, Nataliya Chorna, Iris K. Salgado-Villanueva, Jing Tang, Walter I. Silva Ortiz, Héctor M. Maldonado   +6 more
openaire   +4 more sources

Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells [PDF]

Molecules, 2023
PLK1 is a protein kinase that regulates mitosis and is both an important oncology drug target and a potential antitarget of drugs for the DNA damage response pathway or anti-infective host kinases.
Xuan Yang, Jeffery L. Smith, Michael T. Beck, Jennifer M. Wilkinson, Ani Michaud, James D. Vasta, Matthew B. Robers, Timothy M. Willson   +7 more
doaj   +3 more sources

Temporal phosphoproteomics reveals WEE1-dependent control of 53BP1 pathway

iScience, 2023
Summary: Wee1-like protein kinase (WEE1) restrains activities of cyclin-dependent kinases (CDKs) in S and G2 phase. Inhibition of WEE1 evokes drastic increase in CDK activity, which perturbs replication dynamics and compromises cell cycle checkpoints ...
Valdemaras Petrosius, Jan Benada, Olaf Nielsen, Erwin M. Schoof, Claus Storgaard Sørensen   +4 more
doaj   +2 more sources

Reaction kinetics for the synthesis of an anti-cancer drug (adavosertib) precursor [PDF]

Reaction Chemistry & Engineering
The development of kinetic models which can accurately describe drug synthesis reactions is an important part of process design in the pharmaceutical industry.
Matthew Blair, Mazaher M. Chalchooghi, Robert J. Cox, Dimitrios I. Gerogiorgis   +3 more
openaire   +2 more sources

Multicenter Phase II Trial of the WEE1 Inhibitor Adavosertib in Refractory Solid Tumors Harboring CCNE1 Amplification [PDF]

Journal of Clinical Oncology, 2023
PURPOSE Preclinical cancer models harboring CCNE1 amplification were more sensitive to adavosertib treatment, a WEE1 kinase inhibitor, than models without amplification. Thus, we conducted this phase II study to assess the antitumor activity of adavosertib in patients with CCNE1-amplified, advanced refractory solid tumors. PATIENTS AND METHODS Patients
Siqing Fu, Shuyang Yao, Yuan Yuan, Rebecca A. Previs, Anthony D. Elias, Richard D. Carvajal, Thomas J. George, Ying Yuan, Lihou Yu, Shannon N. Westin, Yan Xing, Ecaterina E. Dumbrava, Daniel D. Karp, Sarina A. Piha-Paul, Apostolia M. Tsimberidou, Jordi Rodon Ahnert, Naoko Takebe, Karen Lu, Khandan Keyomarsi, Funda Meric-Bernstam   +19 more
openaire   +3 more sources

Phase I Study of Adavosertib With Radiotherapy and Temozolomide in Newly Diagnosed Glioblastoma and Intratumoral Drug Levels in Recurrent Glioblastoma [PDF]

Clinical Cancer Research
Abstract Purpose: Adavosertib is an oral small-molecule inhibitor of Wee1. The Adult Brain Tumor Consortium conducted a phase I study evaluating adavosertib in combination with radiation (RT) and temozolomide (TMZ) in patients with newly diagnosed glioblastoma (GBM), as well as a surgical ...
Jennifer Gantchev, Louis B Nabors, David M Peereboom   +2 more
exaly   +5 more sources