From: The Hedgehog signalling pathway in breast development, carcinogenesis and cancer therapy
Classification | Compound (Company) | Origin | Target | Patient population | Â | Development stage | References |
---|---|---|---|---|---|---|---|
Experimental antagonists | Robotnikinin | Macrocycle | HH | - | Â | Preclinical | [88] |
 | Cyclopamine | Veratum californicum | SMO | - |  | Preclinical | |
 | HhAntag | Benzimidazole derivative | SMO | - |  | Preclinical | [5] |
 | Compound5 | Bis-amide class | SMO | - |  | Preclinical | [82] |
 | GANT58 | Thiophene core with four pyridine rings | GLI | - |  | Preclinical | [84] |
 | GANT61 | Hexahydro-pyrimidine derivative | GLI | - |  | Preclinical | [84] |
 | HIP1-4 | Unknown | GLI | - |  | Preclinical | [85] |
 | Zerumbone | Zingiber zerumbet | GLI | - |  | Preclinical | [85] |
 | Arcyriaflavin C | Arcyria ferruginea | GLI | - |  | Preclinical | [85] |
 | Physalin F | Physalis minima | GLI | - |  | Preclinical | [85] |
 | Arsenic trioxide | Arsenic | GLI | - |  | Preclinical | |
Neutralising antibody | 5E1 | Hybridomas | HH | - | Â | Preclinical | [40] |
Small molecules in current clinical trials | GDC-0449/Erivedge/vismodegib(Genentech/Roche/Curis) | Benzimidazole derivate | SMO | Skin | Basal cell carcinoma Basal cell nevus syndrome Breast | Phase I-III (FDA approved) | [77] |
 |  |  |  | CNS/brain/head and neck | Medulloblastoma Glioblastoma |  |  |
 |  |  |  | Aero-and gastrodigestive tract | Lung cancer Oesophagus Stomach Colorectum Pancreas |  |  |
 |  |  |  | Genital tract | Ovarian Prostate |  |  |
 |  |  |  | Blood | Multiple myeloma |  |  |
 |  |  |  | Soft tissue | Chondrosarcoma |  |  |
 | LDE225 (Novartis) | Unknown | SMO | Skin | Basal cell carcinoma Basal cell nevus syndrome Breast | Phase I-II | [77] |
 |  |  |  | CNS/brain/head and neck | Medulloblastoma Glioblastoma Neuroblastoma Astrocytoma |  |  |
 |  |  |  | Aero-and gastrodigestive tract | Lung cancer Colorectum Pancreas |  |  |
 |  |  |  | Blood | Chronic myelogenous leukemia |  |  |
 |  |  |  | Soft tissue | Rhabdomyo-sarcoma |  |  |
 | LEQ506 (Novartis) | Unknown | SMO | Skin | Basal cell carcinoma | Phase I | [77] |
 |  |  |  | CNS/brain/head and neck | Medulloblastoma |  |  |
 | IPI-926 (Infinity Pharma) | Cyclopamine | SMO | Skin | Basal cell carcinoma | Phase I-II | [77] |
 |  |  |  | CNS/head and neck | Head and neck cancer |  |  |
 |  |  |  | Aero-and gastrodigestive tract | Pancreas |  |  |
 |  |  |  | Soft tissue | Chondrosarcoma |  |  |
 | BMS-833923 (BMS/Exelixis) | Unknown | SMO | Skin | Basal cell carcinoma Basal cell nevus syndrome | Phase I-II | [77] |
 |  |  |  | Aero-and gastrodigestive tract | Lung cancer Oesophagus Stomach |  |  |
 |  |  |  | Blood | Acute myeloid leukemia Chronic myelogenous leukemia |  |  |
 | Itraconazole/Sporanox® (Johnson &Johnson) | Triazole antifungal | SMO | Skin | Basal cell carcinoma Breast | Phase I-II (FDA approved) | |
 |  |  |  | CNS/brain/head and neck | Neuroblastoma |  |  |
 |  |  |  | Aero-and gastrodigestive tract | Lung cancer |  |  |
 |  |  |  | Genital tract | Prostate |  |  |
 |  |  |  | Blood | Leukemia Myelodysplastic syndromes |  |  |
 | PF-04449913 (Pfizer) | Unknown | SMO | Blood | Acute myeloid leukemia Myelodysplastic syndrome | Phase I-II | [77] |
 | TAK-441 (Millenium) |  | SMO | Skin | Basal cell carcinoma | Phase I | [77] |