gdc-0941 and Multiple-Myeloma

gdc-0941 has been researched along with Multiple-Myeloma* in 1 studies

Other Studies

1 other study(ies) available for gdc-0941 and Multiple-Myeloma

Article	Year
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. Journal of medicinal chemistry, 2019, 02-28, Volume: 62, Issue:4 Pim kinases have been targets of interest for a number of therapeutic areas. Evidence of durable single-agent efficacy in human clinical trials validated Pim kinase inhibition as a promising therapeutic approach for multiple myeloma patients. Here, we report the compound optimization leading to GDC-0339 (16), a potent, orally bioavailable, and well tolerated pan-Pim kinase inhibitor that proved efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models and has been evaluated as an early development candidate. Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Dogs; Female; Humans; Macaca fascicularis; Madin Darby Canine Kidney Cells; Male; Mice, SCID; Molecular Structure; Multiple Myeloma; Protein Binding; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-pim-1; Pyrazoles; Rats, Sprague-Dawley; Structure-Activity Relationship; Xenograft Model Antitumor Assays	2019

Article

Year

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.

Journal of medicinal chemistry, 2019, 02-28, Volume: 62, Issue:4

Pim kinases have been targets of interest for a number of therapeutic areas. Evidence of durable single-agent efficacy in human clinical trials validated Pim kinase inhibition as a promising therapeutic approach for multiple myeloma patients. Here, we report the compound optimization leading to GDC-0339 (16), a potent, orally bioavailable, and well tolerated pan-Pim kinase inhibitor that proved efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models and has been evaluated as an early development candidate.

Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Dogs; Female; Humans; Macaca fascicularis; Madin Darby Canine Kidney Cells; Male; Mice, SCID; Molecular Structure; Multiple Myeloma; Protein Binding; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-pim-1; Pyrazoles; Rats, Sprague-Dawley; Structure-Activity Relationship; Xenograft Model Antitumor Assays

2019