u-104 and Neoplasms
u-104 has been researched along with Neoplasms* in 2 studies
Trials
1 trial(s) available for u-104 and Neoplasms
| Article | Year |
|---|---|
A Phase 1 Study of SLC-0111, a Novel Inhibitor of Carbonic Anhydrase IX, in Patients With Advanced Solid Tumors.
SLC-0111 is an ureido-substituted benzenesulfonamide small molecule inhibitor of carbonic anhydrase IX. The objectives of this first-in-human Phase 1 study were to determine the safety and tolerability of SLC-0111 in patients with advanced solid tumors and to establish the recommended Phase 2 dose for future clinical investigations.. Using a 3+3 design, dose escalation started at 500 mg oral daily dosing of SLC-0111 in cohort 1 and increased to 1000 and 2000 mg in cohorts 2 and 3. Drug-related adverse events (AEs) were monitored to determine safety and tolerability. Pharmacokinetic analyses assessed plasma concentrations of single and repeated doses of SLC-0111. RECIST 1.1 criteria were used to assess disease progression.. No dose-limiting toxicities were reported and patients dosed at ≤1000 mg exhibited fewer drug-related AEs ≥ grade 3 and fewer AEs such as nausea and vomiting, compared with the 2000-mg cohort. Forty-one percent of patients experienced dose interruptions or discontinuation and the majority (71%) of these occurred in the 2000-mg cohort. Mean Cmax and AUC(0-24) values for single doses were similar at the 1000-mg and 2000-mg dose levels. Mean Tmax and T1/2 values of SLC-0111 were similar after single and repeated dosing. Power-law analysis of Cmax and AUC0-24 showed that exposure to SLC-0111 was generally dose proportional. No objective responses were observed, but stable disease >24 weeks was observed in 2 patients.. SLC-0111 was safe in patients with previously treated, advanced solid tumors. The safety and pharmacokinetic data support 1000 mg/d as the recommended phase 2 dose for SLC-0111. Topics: Adult; Aged; Antigens, Neoplasm; Antineoplastic Agents; Carbonic Anhydrase IX; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Humans; Male; Middle Aged; Neoplasms; Phenylurea Compounds; Sulfonamides | 2020 |
Other Studies
1 other study(ies) available for u-104 and Neoplasms
| Article | Year |
|---|---|
Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII.
In this work, different series of benzothiazole-based sulphonamides Topics: Benzothiazoles; Carbonic Anhydrase Inhibitors; Carbonic Anhydrase IX; Carbonic Anhydrases; Carboxylic Acids; Ethylenes; Humans; Neoplasms; Phenylurea Compounds; Protein Isoforms; Structure-Activity Relationship; Sulfonamides; Zinc | 2022 |