Table 2.
Clinical Development Status of H2S-Releasing Prodrugs
| Company | Drug description | Clinical trials | Indication | Bioavailable |
Orally active |
|---|---|---|---|---|---|
| S content (% weight) | |||||
| Acea Bio (Hangzhou) Co., Ltd. | Fluorapacin (bis(fluorobenzyl) trisulfide) | Phase 1 | Advanced cancer | 10.17 | No |
| Antibe Therapeutics | ATB-346 (naproxen hybrid) | Phase 1 (completed) Phase 2 (completed) Phase 2 (initiated) |
Chronic pain Gastric ulcer Osteoarthritis |
8.75 | Yes |
| Bristol-Myers Squibb | Clopidogrel | FDA approved in 1997 | Antiplatelet | 9.93 | Yes |
| Bristol-Myers Squibb | Zofenopril | FDA approved in 2000 | Hypertension; myocardial infarction | 7.45 | Yes |
| Gicare Pharma, Inc. | GIC-1001 (trimebutine hybrid) | Phase 1 (completed) Phase 2 (completed) |
Pain, cancer, colonic diseases Pain, cancer, colonic diseases |
5.30 | Yes |
| Ikaria Therapeutics (Mallinckrodt Pharmaceuticals) | IK-1001 (aqueous sodium sulfide) | Phase 2 (withdrawn) Phase 2 (terminated) Phase 2 (terminated) |
ST-segment elevation myocardial infarction Coronary artery bypass surgery Renal impairment |
Not applicable | No |
| Sulfagenix, Inc. | SG1002 (sodium polysulthionate) | Phase 1 (completed) Phase 2 (completed) |
Heart failure Male subfertility |
99 | Yes |
| PG-PHARMA, LLC | DBTS | Phase 1 | Stage IV cancer | 11.5 | Yes |
DBTS, dibenzyl trisulphide; FDA, Food and Drug Administration; H2S, hydrogen sulfide.