Table 1.
Hedgehog inhibitors
| Product name | Mechanism of inhibition |
|---|---|
| Research | |
| Arsenic trioxide | Inhibits GLI proteins Degradation of PML-RARA fusion protein110 |
| AY9944 | Inhibits hedgehog pathway, possibly by several mechanisms111 |
| Ciliobrevin A | Hedgehog pathway antagonist, inhibits ciliogenesis112 |
| Cyclopamine | Smoothened antagonist113 |
| GANT58 | Inhibitor of GLI-1-induced transcription114 |
| GANT61 | Inhibitor of GLI-1-and GLI-2-induced transcription114 |
| HPI-1 | Inhibits hedgehog pathway115 |
| Itraconazole | Smoothened antagonist Triazole antifungal116 |
| Jervine | Inhibits hedgehog pathway111 |
| JK184 | Prevents GLI transcriptional activity117 |
| MRT-10 | Smoothened antagonist118 |
| PF-5274857 | Smoothened antagonist119 |
| Robotnikinin | Inhibits SHH120 |
| RU-SKI 43 hydrochloride | Hedgehog acetyltransferase inhibitor121 |
| SANT | Smoothened antagonist122 |
| SMANT hydrochloride | Inhibits SHH-induced accumulation of SMO123 |
| U18666A | Inhibits hedgehog pathway124 |
| Clinical grade | |
| BMS-833923 (Bristol-Myers Squibb; New York City, NY, USA) | Smoothened antagonist125 |
| GDC-0449 (vismodegib) (Genentech; San Francisco, CA, USA) | Specific hedgehog inhibitor FDA approval January 30, 2012126 |
| IPI-926 (saridegib) (Infinity Pharmaceuticals; Cambridge, MA, USA) | Cyclopamine analog127 |
| LDE225 (erismodegib) (Novartis; Basel, Switzerland) | Smoothened antagonist128 |
| PF-04449913 (Pfizer; New York City, NY, USA) | Smoothened antagonist129 |
| TAK-441(Millennium Pharmaceuticals; London, UK) | Smoothened antagonist130 |
Abbreviations: FDA, US Food and Drug Administration; SHH, Sonic hedgehog; SMO, Smoothened.