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. 2015 Jan 16;8:27–38. doi: 10.2147/SCCAA.S58613

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.