Table 3.
Details of small molecules in clinical trials.
| Sl. no. | Drug/company | Dosing | Indications | Current status | Details of recent status |
|---|---|---|---|---|---|
| 1 | CA-170 | 50 mg QD to 1,200 mg | Lymphoma; advanced solid tumors | Phase 2b/3 | In Phase 2 studies, ORR of 30% in classical Hodgkin lymphoma (based on Lugano criteria) and a CBR of >85% at a daily dose of 400 mg and PFS of 19.6 weeks in advanced (stage 4) non-squamous NSCLC (101) CTRI/2017/12/011026 |
| Aurigene/Curis | Phase2b/3 studies: Phase 2b/3 randomized study of CA-170 in patients with non-squamous non-small cell lung cancer CTRI/2020/07/026870 | ||||
| 2 | INCB-086550 | QD (100, 200 mg) or BID (200, 400 mg). | NSCLC urothelial cancer | Phase 2 | Phase 1 Study Exploring the Safety, Tolerability, PK and PD (NCT03762447). |
| Incyte Corp | Renal cell carcinoma | A dose-related 1.2-fold increase in the plasma concentration of soluble target (PD-L1); 3.4-fold increase in IFN- γ; 1.3- and 1.4-fold of CXCL9 and CXCL10, observed post-treatment (116, 086550). | |||
| Hepatocellular carcinoma | Phase 2: Open-label, non-randomized study to evaluate the efficacy and safety (NCT04629339); INCB-086550 will be administered orally twice a day. | ||||
| Melanoma | |||||
| 3 | MX-10181 | Dose not disclosed | Advanced solid tumor; cancer | Phase 1 | In February 2021, an implied trial approval was granted for advanced solid tumor. |
| Maxinovel Pharma | Part 1: Dose escalation, MAX-10181 once or twice daily with dose modifications based on tolerability criteria. | ||||
| Part 2: Dose expansion, Recommended doses from Part 1 (NCT04122339). | |||||
| 4 | GS-4224 | Starting at 400 mg once a day (QD). Subsequent doses of 700 mg QD, 1,000 mg QD, 1,500 mg QD, and 1,000 mg twice a day (BID) | Advanced solid tumor; Hepatitis B virus infection | Phase 1 | In March 2021, Gilead Sciences terminated a phase Ib/II trial to evaluate the safety, tolerability, pharmacokinetics, and efficacy of GS 4224 in patients with advanced solid tumors (NCT04049617). |
| Gilead Sciences | |||||
| 5 | IMMH-010 | Starting at 60 mg QD. Subsequent doses of 120, 240, and 360 mg QD | Malignant neoplasms | Phase 1 | Trial approved in April 2020 and the study is not yet recruited. |
| Tianjin Chasesun Pharmaceutical Co., LTD | To determine MTD and RP2D and to evaluate the effects of food on the pharmacokinetic profiles after single dose of IMMH-010 in patients with advanced solid tumors (NCT04343859). |