المؤلفون: Mar, Nataliya, Zakharia, Yousef, Falcon, Alejandro, Morales-Barrera, Rafael, Mellado, Begona, Duran, Ignacio, Oh, Do-Youn, Williamson, Stephen K, Gajate, Pablo, Arkenau, Hendrik-Tobias, Jones, Robert J, Teo, Min Yuen, Turan, Tolga, McLaughlin, Robert T, Peltier, Hillary M, Chong, Elizabeth, Atluri, Harisha, Dean, James P, Castellano, Daniel

المصدر: Cancers. 15(11)

مصطلحات موضوعية: ibrutinib, paclitaxel, pembrolizumab, urothelial carcinoma, Cancer, Rare Diseases, Clinical Research, Clinical Trials and Supportive Activities, Hematology, 6.1 Pharmaceuticals, Evaluation of treatments and therapeutic interventions, Oncology and Carcinogenesis

الوصف: Ibrutinib is a first-in-class Bruton's tyrosine kinase inhibitor approved for the treatment of various B-cell malignancies and chronic graft-versus-host disease. We evaluated the safety and efficacy of ibrutinib, alone or combined with standard-of-care regimens, in adults with advanced urothelial carcinoma (UC). Once-daily ibrutinib was administered orally at 840 mg (single-agent or with paclitaxel) or at 560 mg (with pembrolizumab). Phase 1b determined the recommended phase 2 dose (RP2D) of ibrutinib, and phase 2 assessed progression-free survival (PFS), overall response rate (ORR), and safety. Thirty-five, eighteen, and fifty-nine patients received ibrutinib, ibrutinib plus pembrolizumab, and ibrutinib plus paclitaxel at the RP2D, respectively. Safety profiles were consistent with those of the individual agents. The best-confirmed ORRs were 7% (two partial responses) with single-agent ibrutinib and 36% (five partial responses) with ibrutinib plus pembrolizumab. Median PFS was 4.1 months (range, 1.0-37.4+) with ibrutinib plus paclitaxel. The best-confirmed ORR was 26% (two complete responses). In previously treated patients with UC, ORR was higher with ibrutinib plus pembrolizumab than with either agent alone (historical data in the intent-to-treat population). ORR with ibrutinib plus paclitaxel was greater than historical values for single-agent paclitaxel or ibrutinib. These data warrant further evaluation of ibrutinib combinations in UC.

وصف الملف: application/pdf

الوصول الحر: https://escholarship.org/uc/item/05b652c2Test

المؤلفون: Bembenek, Scott D., Venkatesan, Hariharan, Peltier, Hillary M., Rosen, Mark D., Barrett, Terrance D., Kanelakis, Kimon C., Palomino, Heather L., Brondstetter, Theresa I., Mirzadegan, Taraneh, Rabinowitz, Michael H.

المصدر: ACS Omega ; volume 4, issue 4, page 6703-6708 ; ISSN 2470-1343 2470-1343

مصطلحات موضوعية: General Chemical Engineering, General Chemistry

الإتاحة: https://doi.org/10.1021/acsomega.9b00199Test

المؤلفون: Patel, Meena V., Peltier, Hillary M., Matulenko, Mark A., Koenig, John R., C. Scanio, Marc J., Gum, Rebecca J., El-Kouhen, Odile F., Fricano, Meagan M., Lundgaard, Greta L., Neelands, Torben, Zhang, Xu-Feng, Zhan, Cenchen, Pai, Madhavi, Ghoreishi-Haack, Nayereh, Hudzik, Thomas, Gintant, Gary, Martin, Ruth, McGaraughty, Steve, Xu, Jun, Bow, Daniel, Kalvass, John C., Kym, Philip R., DeGoey, David A., Kort, Michael E.

المصدر: Bioorganic & Medicinal Chemistry ; volume 63, page 116743 ; ISSN 0968-0896

مصطلحات موضوعية: Organic Chemistry, Clinical Biochemistry, Drug Discovery, Pharmaceutical Science, Molecular Biology, Molecular Medicine, Biochemistry

الإتاحة: https://doi.org/10.1016/j.bmc.2022.116743Test
https://api.elsevier.com/content/article/PII:S0968089622001353?httpAccept=text/xmlTest
https://api.elsevier.com/content/article/PII:S0968089622001353?httpAccept=text/plainTest

مستخلص: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity. [chemical expression included]

المؤلفون: Cusack, Kevin P., Koolman, Hannes F., Lange, Udo E.W., Peltier, Hillary M., Piel, Isabel, Vasudevan, Anil

المصدر: Bioorganic & Medicinal Chemistry Letters ; volume 23, issue 20, page 5471-5483 ; ISSN 0960-894X

مصطلحات موضوعية: Organic Chemistry, Clinical Biochemistry, Drug Discovery, Pharmaceutical Science, Molecular Biology, Molecular Medicine, Biochemistry

الإتاحة: https://doi.org/10.1016/j.bmcl.2013.08.003Test
https://api.elsevier.com/content/article/PII:S0960894X13009323?httpAccept=text/xmlTest
https://api.elsevier.com/content/article/PII:S0960894X13009323?httpAccept=text/plainTest

مستخلص: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity. [chemical expression included]

المؤلفون: Cusack, Kevin P., Koolman, Hannes F., Lange, Udo E. W., Peltier, Hillary M., Piel, Isabel, Vasudevan, Anil

المصدر: ChemInform ; volume 44, issue 51 ; ISSN 0931-7597 1522-2667

الوصف: Review: about 100 refs.

الإتاحة: https://doi.org/10.1002/chin.201351270Test

المؤلفون: Rosen, Mark D., Venkatesan, Hariharan, Peltier, Hillary M., Bembenek, Scott D., Kanelakis, Kimon C., Zhao, Lucy X., Leonard, Barry E., Hocutt, Frances M., Wu, Xiaodong, Palomino, Heather L., Brondstetter, Theresa I., Haugh, Peter V., Cagnon, Laurence, Yan, Wen, Liotta, Lisa A., Young, Andrew, Mirzadegan, Tara, Shankley, Nigel P., Barrett, Terrance D., Rabinowitz, Michael H.

المصدر: ACS Medicinal Chemistry Letters ; volume 1, issue 9, page 526-529 ; ISSN 1948-5875 1948-5875

الإتاحة: https://doi.org/10.1021/ml100198yTest

المؤلفون: Tanuwidjaja, Jessica, Peltier, Hillary M., Lewis, Jared C., Schenkel, Laurie B., Ellman, Jonathan A.

المصدر: ChemInform ; volume 39, issue 13 ; ISSN 0931-7597 1522-2667

الوصف: ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

الإتاحة: https://doi.org/10.1002/chin.200813041Test

المؤلفون: Patterson, Andrew W., Peltier, Hillary M., Ellman, Jonathan A.

المصدر: The Journal of Organic Chemistry ; volume 73, issue 12, page 4362-4369 ; ISSN 0022-3263 1520-6904

مصطلحات موضوعية: Organic Chemistry

الإتاحة: https://doi.org/10.1021/jo800384xTest