Table 3.
Therapeutic application of cGAS and STING activators
| Target | Activator | Target diseases | Phase | Clinical trial NCT code | |
|---|---|---|---|---|---|
| cGAS | Manganese | Unresectable/metastatic solid tumors or lymphomas | Phase I | NCT03991559 | |
| Micronuclei | Senescence and various human cancer cells | Preclinical | |||
| STING | Cyclic Dinucleotides (CDNs) | 3′3′-cyclic AIMP | Hepatocellular carcinoma | Preclinical | |
| BI 1387446 (BI-STING) | Advanced solid tumors | Phase I | NCT04147234 | ||
| BMS-986301 | Advanced solid tumors | Phase I | NCT03956680 | ||
| E7766 | Advanced solid tumors or lymphomas | Phase Ia/Ib | NCT04144140 | ||
| exoSTING (CDK-002) | Advanced/metastatic, recurrent, injectable solid tumors | Phase I/ II | NCT04592484 | ||
| GSK532 | Colorectal carcinoma | Preclinical | |||
| IMSA101 (GB492) | Refractory malignancies | Phase I/ II | NCT04020185 | ||
| JNJ-67544412 (JNJ-4412) | Subcutaneous syngeneic murine tumor models | Preclinical | |||
| MIW815 (ADU-S100, ML RR-S2 CDA) | Advanced/metastatic solid tumors or lymphomas | Phase I | NCT03172936 | ||
| Advanced/metastatic solid tumors or lymphomas | Phase I | NCT02675439 | |||
| PD-L1 positive recurrent or metastatic HNSCC | phases II | NCT03937141 | |||
| MK-1454 | Advanced/metastatic solid tumors or lymphomas | Phase I | NCT03010176 | ||
| Metastatic or unresectable, recurrent HNSCC | phase II | NCT04220866 | |||
| Nano-STING agonist-decorated microrobot | Murine tumor models | Preclinical | |||
| SB11285 | Advanced solid tumors | Phase Ia/Ib | NCT04096638 | ||
| Non-Cyclic Dinucleotides | ALG-031048 | Colorectal carcinoma | Preclinical | ||
| CRD5500 (LB-061) | Colorectal carcinoma | Preclinical | |||
| CS-1018, CS-1020 and CS-1010 | Colon adenocarcinoma and melanoma | Preclinical | |||
| GSK3745417 | Advanced solid tumors | Phase I | NCT03843359 | ||
| JNJ- ‘6196 | Murine tumor models (not specified) | Preclinical | |||
| MK-2118 | Advanced/metastatic solid tumors or lymphomas | Phase I | NCT03249792 | ||
| MSA-1 | Colorectal carcinoma | Preclinical | |||
| MSA-2 | Colon adenocarcinoma and melanoma | Preclinical | |||
| NEs@STING-Mal-NP | TNBC tumor | Preclinical | |||
| Ryvu’s activators | Colorectal carcinoma | Preclinical | |||
| SAL-LNP | SARS-CoV-2 infection | Preclinical | |||
| Selvita activators | In vitro assays for STING activators | Preclinical | |||
| SNX281 | Advanced solid tumors or lymphomas | Phase I | NCT04609579 | ||
| TAK-676 | Advanced solid tumors | Phase I | NCT04420884 | ||
| TTI-10001 | Multiple syngeneic murine tumor models | Preclinical | |||
| Ectonucleotide pyrophosphatase/phosphodiesterase 1(ENPP1) Inhibitor | MV-626 | pancreatic adenocarcinoma tumors | Preclinical | ||
| SR-8314/ SR-8291 | Syngeneic murine tumor models | Preclinical | |||
| SR-8541A | In vitro assays for STING activators | Preclinical | |||
| Others | Bacterial-based activators | STACT | Colorectal carcinoma and melamoma | Preclinical | |
| SYNB1891 | Advanced solid tumors or lymphomas | Phase I | NCT04167137 | ||
| Immune stimulating antibody conjugate (ISAC) | ADC XMT-2056 | Advanced/recurrent solid tumors | Phase I | NCT05514717 | |
| TAK-500 | Advanced or metastatic solid tumors | Phase Ia/Ib | NCT05070247 | ||