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DRUG:

Erivedge (vismodegib)

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Other names: GDC 0449, GDC-0449, GDC0449, R 3616, R3616, RG3616, RG 3616, RO5450815, RO-5450815, RO 5450815, R-3616, RG-3616
Company:
Curis, Roche
Drug class:
Hedgehog cell-signalling pathway inhibitor
6d
Ldha Regulates Osteosarcoma Lung Metastasis through Hedgehog Signaling. (PubMed, Cancer Res Commun)
Consistently, pharmacological inhibition of Hedgehog signaling using vismodegib suppressed cell migration, invasion, and lung metastases in murine osteosarcoma cells. In human osteosarcoma cells, LDHA silencing downregulated Hedgehog signaling, and inhibition of Hedgehog signaling suppressed cell migration and invasion. These findings highlight the involvement of the Ldha-Hedgehog signaling axis in osteosarcoma lung metastases, providing insights into its molecular mechanisms and potential therapeutic targets.
Journal
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LDHA (Lactate dehydrogenase A)
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Erivedge (vismodegib)
14d
Improving public cancer care by implementing precision medicine in Norway (2023-507894-16-00)
P1/2, N=1000, Recruiting, Oslo University Hospital HF | N=6000 --> 1000
Enrollment change
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Avastin (bevacizumab) • Lynparza (olaparib) • Mekinist (trametinib) • Tecentriq (atezolizumab) • Zelboraf (vemurafenib) • Tafinlar (dabrafenib) • Rozlytrek (entrectinib) • imatinib • Alecensa (alectinib) • Cotellic (cobimetinib) • bortezomib • Piqray (alpelisib) • Zejula (niraparib) • Retevmo (selpercatinib) • Zykadia (ceritinib) • fulvestrant • Jemperli (dostarlimab-gxly) • Pemazyre (pemigatinib) • Tepmetko (tepotinib) • Tabrecta (capmatinib) • dexamethasone • Erivedge (vismodegib) • melphalan • dactinomycin • Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) • hydroxyurea
21d
New P1/2 trial
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Keytruda (pembrolizumab) • Lynparza (olaparib) • Mekinist (trametinib) • Xalkori (crizotinib) • erlotinib • Tafinlar (dabrafenib) • Vitrakvi (larotrectinib) • gemcitabine • paclitaxel • 5-fluorouracil • capecitabine • Retevmo (selpercatinib) • albumin-bound paclitaxel • oxaliplatin • irinotecan • Pemazyre (pemigatinib) • axitinib • Erivedge (vismodegib) • leucovorin calcium • Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf)
2ms
Structure Merging Approach Leads to New Dual Potent and Selective USP25/USP28 Inhibitors. (PubMed, J Med Chem)
In this study, we present a strategy that merges structural features of the previously identified inhibitors AZ1 and vismodegib to develop a new class of potent dual inhibitors...Moreover, a suitable negative control has also been identified, supporting the validity of the observed effects in cellular assays. These results highlight the potential of these compounds to serve as advanced chemical probes for dual USP25/USP28 inhibition and as candidates for further therapeutic development.
Journal
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USP25 (Ubiquitin Specific Peptidase 25)
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Erivedge (vismodegib)
2ms
Metastatic Basal Cell Carcinoma With Unusual Molecular Genetics Findings. (PubMed, Clin Case Rep)
The patient was managed with complete excision of the lesion, along with a neck dissection for level V lymph nodes, and adjuvant chemotherapy with Vismodegib...However, considering the possibility of metastasis, the patient is being followed up by a multi-disciplinary team (MDT) for evaluation of level IIB cervical lymph nodes. This case highlights the diagnostic and therapeutic challenges that may arise in rare cases of BCC with metastasis.
Journal
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CDKN2B (Cyclin Dependent Kinase Inhibitor 2B) • HMGA2 (High mobility group AT-hook 2)
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Erivedge (vismodegib)
3ms
Trial completion date
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BCL2 (B-cell CLL/lymphoma 2)
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erlotinib • gemcitabine • Erivedge (vismodegib)
3ms
Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (clinicaltrials.gov)
P2, N=720, Recruiting, Canadian Cancer Trials Group | Trial primary completion date: Jan 2026 --> Dec 2026
Trial primary completion date • Tumor mutational burden • Pan tumor
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BRAF (B-raf proto-oncogene)
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Opdivo (nivolumab) • Herceptin (trastuzumab) • Lynparza (olaparib) • Xalkori (crizotinib) • erlotinib • Yervoy (ipilimumab) • Ibrance (palbociclib) • dasatinib • Zelboraf (vemurafenib) • sunitinib • Perjeta (pertuzumab) • Cotellic (cobimetinib) • bosutinib • Tukysa (tucatinib) • temsirolimus • axitinib • Erivedge (vismodegib)
3ms
Vismodegib and Atezolizumab for the Treatment of Recurrent or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
P1, N=24, Recruiting, Dwight Owen | Suspended --> Recruiting | Trial completion date: Dec 2026 --> Dec 2027
Enrollment open • Trial completion date
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EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • ALK (Anaplastic lymphoma kinase) • CD4 (CD4 Molecule)
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Tecentriq (atezolizumab) • Erivedge (vismodegib)
3ms
Actin-related protein 6 regulates the Hedgehog signaling pathway: Molecular basis for stemness maintenance of hepatoma cells. (PubMed, Cytojournal)
Vismodegib reversed the promoting effect of ACTR6 on the Hh signaling pathway and stem-related proteins in cells. ACTR6 regulates the molecular basis of stemness maintenance of liver cancer cells through the Hh signaling pathway and promotes the occurrence of liver cancer. This study provides possible targets for the clinical treatment of liver cancer.
Journal
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PTCH1 (Patched 1) • YBX1 (Y-Box Binding Protein 1) • NANOG (Nanog Homeobox) • SHH (Sonic Hedgehog Signaling Molecule) • TCF4 (Transcription Factor 4)
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Erivedge (vismodegib)
4ms
The Therapeutic Effect and Mechanism of Vismodegib on COPD: Focusing on NETs and Macrophage Polarization. (PubMed, Chem Biol Drug Des)
Vismodegib may alleviate inflammation and tissue damage in COPD by inhibiting NETs-mediated M1 polarization of macrophages. This study is the first to propose the targeting of NET-driven macrophage polarization via Hedgehog inhibition as a novel therapeutic strategy for COPD, providing a new mechanistic framework for drug repurposing.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL17A (Interleukin 17A) • IL1B (Interleukin 1, beta) • MPO (Myeloperoxidase)
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Erivedge (vismodegib)
4ms
Sonic Hedgehog Pathway Modulation in Medulloblastoma: Focus on Vismodegib (GDC-0449). (PubMed, Dev Neurobiol)
Prospects encompass the enhancement of drug delivery methods, the integration of SHH inhibitors with alternative therapeutics, and the advancement of next-generation inhibitors to surmount resistance. Hence, these developments offer potential for improving outcomes in SHH-MB while reducing side effects, especially in pediatric populations.
Review • Journal
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PTCH1 (Patched 1) • SMO (Smoothened Frizzled Class Receptor)
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Erivedge (vismodegib)
4ms
A Case Report of Promising Response to Combination Therapy With an Immune Checkpoint Inhibitor (Pembrolizumab) and Multi-Targeted Tyrosine Kinase Inhibitor (Pazopanib) in Metastatic De-Differentiated Chondrosarcoma. (PubMed, Cancer Rep (Hoboken))
This case report is a valuable example of promising emerging systemic therapies for advanced DDCS, where the present standard of care lacks a repertoire of effective therapies.
Journal • Checkpoint inhibition • PD(L)-1 Biomarker • IO biomarker
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IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • PTCH1 (Patched 1)
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Keytruda (pembrolizumab) • pazopanib • Erivedge (vismodegib)