Results 11 to 20 of about 1,361 (136)

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

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 & Disease, 2023
AbstractDespite 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. Here, we show that the lysine methyltransferase SETD8 is overexpressed in 50% of high-grade gliomas.
Della Monica, Rosa, Buonaiuto, Michela, Cuomo, Mariella, Pagano, Cristina, Trio, Federica, Costabile, Davide, de Riso, Giulia, Cicala, Francesca Sveva, Raia, Maddalena, Franca, Raduan Ahmed, Del Basso De Caro, Marialaura, Sorrentino, Domenico, Navarra, Giovanna, Coppola, Laura, Tripodi, Lorella, Pastore, Lucio, Hench, Juergen, Frank, Stephan, Schonauer, Claudio, Catapano, Giuseppe, Bifulco, Maurizio, Chiariotti, Lorenzo, Visconti, Roberta   +22 more
openaire   +5 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

Inhibition of WEE1 Is Effective in TP53- and RAS-Mutant Metastatic Colorectal Cancer: A Randomized Trial (FOCUS4-C) Comparing Adavosertib (AZD1775) With Active Monitoring [PDF]

, 2021
PURPOSE Outcomes in RAS-mutant metastatic colorectal cancer (mCRC) remain poor and patients have limited therapeutic options. Adavosertib is the first small-molecule inhibitor of WEE1 kinase.
Richman, SD, de Winton, E, Jones, R, Graham, J, Collinson, F, Brown, E, Seymour, M, Quirke, P, Yates, E, Maughan, TS, Brown, LC, Domingo, E, Braun, M, Kaplan, R, Seligmann, JF, Fisher, DJ, Butler, R, FOCUS4 Trial Investigators, ., Humphrey, TC, Parmar, M, Blake, A, Adams, RA, Wilson, RH   +22 more
core   +6 more sources

Technoeconomically and environmentally optimal design of reactors and separators in pharmaceutical manufacturing of adavosertib and flurbiprofen

The development of cost-optimal yet sustainable manufacturing processes is a growing priority in the pharmaceutical industry, with many institutions hoping to become carbon neutral in the near future. However, the majority of research and development (R&D) activities within the sector still rely heavily on the use of experimental trials, making the
Blair, Matthew William
openaire   +3 more sources

Adavosertib [PDF]

, 2020
openaire   +2 more sources

WEE1 Inhibition as a Novel Therapeutic Strategy in Cutaneous T-Cell Lymphoma. [PDF]

Cancers (Basel)
Background/Objectives: Cutaneous T-cell lymphomas (CTCL), most commonly mycosis fungoides and Sézary syndrome, are rare non-Hodgkin lymphomas. Advanced disease responds poorly to current treatments, highlighting the need for new molecularly targeted ...
Özistanbullu D, Bahrami K, Doll M, Reichenbach G, Pöschl SM, Wilhelm R, Stege H, Zöller N, Winkler L, Jäger M, Nicolay JP, Quist SR, Kaufmann R, Meissner M, Schilling B, Kleemann J, Cinatl J, Kippenberger S.   +17 more
europepmc   +3 more sources

Phase 2 study of Wee1 inhibitor adavosertib in recurrent uterine carcinosarcoma. [PDF]

Gynecol Oncol Rep
Uterine carcinosarcoma (UCS) is a rare but aggressive tumor with high rates of recurrence and poor prognosis, and novel therapies are urgently needed. P53 mutations are identified in over 90% of cases, and other cell cycle alterations are commonly found indicating potential vulnerability to Wee1 kinase inhibition.
Cham S, Xiong N, Tayob N, Krasner C, Wright AA, Lee EK, Sawyer H, Mathews C, Konstantinopoulos PA, Matulonis UA, Liu JF.   +10 more
europepmc   +4 more sources