Table 2.
Representative clinical trials targeting tumor AP inhibitory mechanismsa
| NCT number | Phase | Targeted cancer | Design | Primary endpoint | Severe adverse event (grade ≥3) | Status | Registration | Trial report |
|---|---|---|---|---|---|---|---|---|
| NCT05553834 v | 2 | Metastatic lung cancer | Single arm, open label | Response rate | N/A | Recruiting | USA | No results |
| NCT05128539 vi | 1 | Advanced cancers | Single arm, open label | 1. AE, SAE, irAE (3 years); 2. DLTs (3 years); 3. MTD (1 year); 4. RDE (1 year) | N/A | Recruiting | China | No results |
| NCT05467748 i | 1b/2 | Advanced non-small cell lung cancer | Single arm, open label | 1. ORR (2 years); 2. S&T (2 years) | N/A | Not yet recruiting | USA | No results |
| NCT06022757 ii | 1b/2 | Advanced solid tumors | Single arm, open label | Phase 1b. RP2D (21 days); Phase 2. ORR (Phase 2) (baseline, every 9 weeks in the first 54 weeks, then every 12 weeks thereafter until confirmed disease) | N/A | Not yet recruiting | N/A | No results |
| NCT05448677 iv | 2b | Unresectable hepatocellular carcinoma | Randomized | PFS (36 months) | N/A | Recruiting | France | No results |
| NCT04214418 iii | 1/2 | Advanced cancers with KRAS mutation | Single arm, open label | Phase 1: MTD (16 weeks); Phase 2: MTD (based on Phase 1) | 1. Grade 3 or higher TRAEs: 50%; 2. Grade 5 TRAEs: 7% | Active, not recruiting | USA | [72] |
| NCT04944888 vii | 1 | Advanced relapsed or refractory hematological malignancies and previously treated solid tumors | Single arm, open label | Number of subjects occurring treatment-related adverse events (90 days after the last dose) | N/A | Completed | China | No results |
| NCT05082259 viii | 1 | Advanced cancer, cervical cancer, triple-negative breast cancer | Single arm, open label | 1. MTD RP2D (12 months); 2. S&T (12 months); 3. Preliminary antitumor activity evaluation (in Part B) (24 months) | N/A | Recruiting | UK | No results |
| NCT04122625 ix | 1/2 | Specific solid tumors | Single arm, open label | 1. DLTs (28 days); 2. Part B: ORR (2.05 years) | Part B: grade ≥3 TRAEs: 25.7% | Completed | France, Spain, USA | [73] |
| NCT04396457 x | 2 | Non-squamous non-small cell lung cancer | Single arm, open label | ORR (3 years) | N/A | Active, not recruiting | Japan | No results |
| NCT02260440 xi | 2 | Chemotherapy refractory metastatic colorectal cancer | Single arm, open label | ORR (14 months) | Grade ≥3 TRAEs: 2.5% | Completed | USA | [74] |
| NCT02437136 xii | 1b/2 | Non-small cell lung cancer, melanoma, and mismatch repair-proficient colorectal cancer | Single arm, open label | 1. S&T (3–4 months); 2. ORR (1–2 years) | Grade ≥3 TRAEs: 18.8% | Completed | USA | [75] |
| NCT04216953 xiii | 1/2 | Locally advanced and/or metastatic soft tissue sarcoma | Single arm, open label | PFR (16 weeks) | N/A | Recruiting | France | No results |
| NCT05422794 xiv | 1 | Metastatic triple-negative breast cancer | Single arm, open label | 1. MTD (28 days); 2. RP2D (28 days); 3. IAE (3 years) | N/A | Recruiting | USA | No results |
| NCT04946370 xv | 1/2 | Progressive metastatic castration-resistant prostate cancer | Randomized | 1. DLT (12 weeks); 2. RP2D (12 weeks); 3. CRR (100 months) | N/A | Recruiting | USA | No results |
a
Abbreviations: AE, adverse event; CRR, composite response rate; DCR, disease control rate; DLT, dose-limiting toxicity; IAE, incidence of adverse events; irAE, immune-related adverse event; MTD, maximum tolerated dose; ORR, objective response rate; PFR, progression-free rate; PFS, progression-free survival; RDE, recommended dose for extension; RP2D, recommended Phase 2 dose; S&T, safety and tolerability; SAE, serious adverse event; TRAE, treatment-related adverse event.