Vismodegib (BioDeep_00000392555)
代谢物信息卡片
vismodegib(GDC-0449)
化学式: C19H14Cl2N2O3S (420.0102154)
中文名称: 维莫地尼
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CS(=O)(=O)C1=CC(=C(C=C1)C(=O)NC2=CC(=C(C=C2)Cl)C3=CC=CC=N3)Cl
InChI: InChI=1S/C19H14Cl2N2O3S/c1-27(25,26)13-6-7-14(17(21)11-13)19(24)23-12-5-8-16(20)15(10-12)18-4-2-3-9-22-18/h2-11H,1H3,(H,23,24)
描述信息
L - Antineoplastic and immunomodulating agents > L01 - Antineoplastic agents > L01X - Other antineoplastic agents > L01XJ - Hedgehog pathway inhibitors
C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C188731 - Hedgehog Pathway Inhibitor
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor
同义名列表
2 个代谢物同义名
数据库引用编号
8 个数据库交叉引用编号
- ChEBI: CHEBI:66903
- KEGGdrug: D09992
- PubChem: 24776445
- Metlin: METLIN85191
- DrugBank: DB08828
- ChEMBL: CHEMBL473417
- CAS: 879085-55-9
- PMhub: MS000242829
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Yuting Zhang, Weijuan Xin, Xiaozhi Hu, Hanqi Wang, Xiaomiao Ye, Caili Xu, Yanyang Nan, Zhengyu Wu, Dianwen Ju, Jiajun Fan. Inhibition of Hedgehog signaling ameliorates foam cell formation by promoting autophagy in early atherosclerosis.
Cell death & disease.
2023 Nov; 14(11):740. doi:
10.1038/s41419-023-06270-5. [PMID: 37963874] - Yixing Yao, Tianyuan Li, Tingting Yu, Xin Yang, Yue Wang, Jing Cai, Steven Y Cheng, Chen Liu, Shen Yue. Hedgehog signal activates AMPK via Smoothened to promote autophagy and lipid degradation in hepatocytes.
Biochemistry and cell biology = Biochimie et biologie cellulaire.
2023 08; 101(4):284-293. doi:
10.1139/bcb-2022-0345. [PMID: 36821837] - Huanxian Wu, Lishun Zhang, Boyu Chen, Baofang Ou, Jiahuan Xu, Nannan Tian, Danni Yang, Yangcheng Ai, Qianqing Chen, Dongling Quan, Tingting Zhang, Lin Lv, Yuanxin Tian, Jiajie Zhang, Shaoyu Wu. B13, a well-tolerated inhibitor of hedgehog pathway, exhibited potent anti-tumor effects against colorectal carcinoma in vitro and in vivo.
Bioorganic chemistry.
2023 Mar; 135(?):106488. doi:
10.1016/j.bioorg.2023.106488. [PMID: 36989734] - Mrinal M Gounder, Evan Rosenbaum, Nian Wu, Mark A Dickson, Tahir N Sheikh, Sandra P D'Angelo, Ping Chi, Mary Lou Keohan, Joseph P Erinjeri, Cristina R Antonescu, Narasimhan Agaram, Meera R Hameed, Moriah Martindale, Robert A Lefkowitz, Aimee M Crago, Sam Singer, William D Tap, Naoko Takebe, Li-Xuan Qin, Gary K Schwartz. A Phase Ib/II Randomized Study of RO4929097, a Gamma-Secretase or Notch Inhibitor with or without Vismodegib, a Hedgehog Inhibitor, in Advanced Sarcoma.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2022 04; 28(8):1586-1594. doi:
10.1158/1078-0432.ccr-21-3874. [PMID: 35110418] - Michael Migden, Aaron S Farberg, Reinhard Dummer, Nicholas Squittieri, C William Hanke. A Review of Hedgehog Inhibitors Sonidegib and Vismodegib for Treatment of Advanced Basal Cell Carcinoma.
Journal of drugs in dermatology : JDD.
2021 02; 20(2):156-165. doi:
10.36849/jdd.5657. [PMID: 33538567] - Duhyeong Hwang, Taylor Dismuke, Andrey Tikunov, Elias P Rosen, John R Kagel, Jacob D Ramsey, Chaemin Lim, William Zamboni, Alexander V Kabanov, Timothy R Gershon, Marina Sokolsky-Papkov PhD. Poly(2-oxazoline) nanoparticle delivery enhances the therapeutic potential of vismodegib for medulloblastoma by improving CNS pharmacokinetics and reducing systemic toxicity.
Nanomedicine : nanotechnology, biology, and medicine.
2021 02; 32(?):102345. doi:
10.1016/j.nano.2020.102345. [PMID: 33259959] - Uffe Høgh Olesen, Gael Clergeaud, Kristoffer Kjærgaard Hendel, Kelvin Yeung, Catharina Margrethe Lerche, Thomas Lars Andresen, Merete Haedersdal. Enhanced and Sustained Cutaneous Delivery of Vismodegib by Ablative Fractional Laser and Microemulsion Formulation.
The Journal of investigative dermatology.
2020 10; 140(10):2051-2059. doi:
10.1016/j.jid.2020.01.032. [PMID: 32135181] - Michael J Dolton, Po-Chang Chiang, Fang Ma, Jin Y Jin, Yuan Chen. A Physiologically Based Pharmacokinetic Model of Vismodegib: Deconvoluting the Impact of Saturable Plasma Protein Binding, pH-Dependent Solubility and Nonsink Permeation.
The AAPS journal.
2020 09; 22(5):117. doi:
10.1208/s12248-020-00503-7. [PMID: 32875428] - Alessia Villani, Gabriella Fabbrocini, Claudia Costa, Massimiliano Scalvenzi. Patients with advanced basal cell carcinomas in treatment with sonic hedgehog inhibitors during the coronavirus disease 2019 (COVID-19) period: Management and adherence to treatment.
Journal of the American Academy of Dermatology.
2020 06; 82(6):e205. doi:
10.1016/j.jaad.2020.03.057. [PMID: 32244017] - Bonan Zhang, Hong Xu, Yi Zhang, Xue Yi, Guizhen Zhang, Xin Zhang, Dingjie Xu, Xuemin Gao, Shifeng Li, Ying Zhu, Hui Zhang, Zhongqiu Wei, Shumin Li, Lijuan Zhang, Ruimin Wang, Fang Yang. Targeting the RAS axis alleviates silicotic fibrosis and Ang II-induced myofibroblast differentiation via inhibition of the hedgehog signaling pathway.
Toxicology letters.
2019 Oct; 313(?):30-41. doi:
10.1016/j.toxlet.2019.05.023. [PMID: 31181250] - Jennifer C. Tang, Larry Buckel, C. William Hanke. Histopathology of Basal Cell Carcinoma After Treatment With Vismogedib.
Journal of drugs in dermatology : JDD.
2019 Feb; 18(2):136-138. doi:
NULL. [PMID: 30794363] - Uffe H Olesen, Gael Clergeaud, Catharina M Lerche, Thomas L Andresen, Merete Haedersdal. Topical delivery of vismodegib using ablative fractional laser and micro-emulsion formulation in vitro.
Lasers in surgery and medicine.
2019 01; 51(1):79-87. doi:
10.1002/lsm.23013. [PMID: 30152536] - Andrea Sbrana, Andrea Antonuzzo, Luca Galli, Elisa Biasco, Gianna Musettini, Federico Paolieri, Sergio Ricci. A case of a patient with severe renal failure on hemodialysis treated with vismodegib for relapsing basal cell carcinoma.
Tumori.
2018 Dec; 104(6):NP2-NP4. doi:
10.1177/0300891618778952. [PMID: 29895211] - Claire Pressiat, Huu-Hien Huynh, Alain Plé, Hélène Sauvageon, Isabelle Madelaine, Cécile Chougnet, Christine Le Maignan, Samia Mourah, Lauriane Goldwirt. Development and Validation of a Simultaneous Quantification Method of Ruxolitinib, Vismodegib, Olaparib, and Pazopanib in Human Plasma Using Liquid Chromatography Coupled With Tandem Mass Spectrometry.
Therapeutic drug monitoring.
2018 06; 40(3):337-343. doi:
10.1097/ftd.0000000000000497. [PMID: 29474275] - Virender Kumar, Vaibhav Mundra, Yang Peng, Yingzhe Wang, Chalet Tan, Ram I Mahato. Pharmacokinetics and biodistribution of polymeric micelles containing miRNA and small-molecule drug in orthotopic pancreatic tumor-bearing mice.
Theranostics.
2018; 8(15):4033-4049. doi:
10.7150/thno.24945. [PMID: 30128034] - P Koelblinger, R Dummer, M Laimer, S Hecht, J W Bauer, A Gaggl, A Kugler. Vismodegib for recurrent locally destructive basal cell carcinoma in a renal transplant patient.
Journal of the European Academy of Dermatology and Venereology : JEADV.
2018 Jan; 32(1):e7-e8. doi:
10.1111/jdv.14430. [PMID: 28646606] - Jochen Dutzmann, Alexander Koch, Simona Weisheit, Kristina Sonnenschein, Laura Korte, Marco Haertlé, Thomas Thum, Johann Bauersachs, Daniel G Sedding, Jan-Marcus Daniel. Sonic hedgehog-dependent activation of adventitial fibroblasts promotes neointima formation.
Cardiovascular research.
2017 Nov; 113(13):1653-1663. doi:
10.1093/cvr/cvx158. [PMID: 29088375] - Guiquan Jia, Sanjay Chandriani, Alexander R Abbas, Daryle J DePianto, Elsa N N'Diaye, Murat B Yaylaoglu, Heather M Moore, Ivan Peng, Jason DeVoss, Harold R Collard, Paul J Wolters, Jackson G Egen, Joseph R Arron. CXCL14 is a candidate biomarker for Hedgehog signalling in idiopathic pulmonary fibrosis.
Thorax.
2017 09; 72(9):780-787. doi:
10.1136/thoraxjnl-2015-207682. [PMID: 28250200] - Ghassan K Abou-Alfa, Lionel D Lewis, Patricia LoRusso, Michael Maitland, Priya Chandra, Sravanthi Cheeti, Dawn Colburn, Sarah Williams, Brian Simmons, Richard A Graham. Pharmacokinetics and safety of vismodegib in patients with advanced solid malignancies and hepatic impairment.
Cancer chemotherapy and pharmacology.
2017 Jul; 80(1):29-36. doi:
10.1007/s00280-017-3315-8. [PMID: 28523596] - Rinku Dutta, Virender Kumar, Yang Peng, Ruby E Evande, Jean L Grem, Ram I Mahato. Pharmacokinetics and Biodistribution of GDC-0449 Loaded Micelles in Normal and Liver Fibrotic Mice.
Pharmaceutical research.
2017 03; 34(3):564-578. doi:
10.1007/s11095-016-2081-3. [PMID: 27995525] - Douglas Fife, Marko A Laitinen, David J Myers, Pamela B Landsteiner. Vismodegib Therapy for Basal Cell Carcinoma in an 8-Year-Old Chinese Boy with Xeroderma Pigmentosum.
Pediatric dermatology.
2017 Mar; 34(2):163-165. doi:
10.1111/pde.13080. [PMID: 28297142] - Gang Liu, Ding Xue, Jun Yang, Juan Wang, Xiaohua Liu, Wenjing Huang, Jie Li, Ya-Qiu Long, Wenfu Tan, Ao Zhang. Design, Synthesis, and Pharmacological Evaluation of 2-(2,5-Dimethyl-5,6,7,8-tetrahydroquinolin-8-yl)-N-aryl Propanamides as Novel Smoothened (Smo) Antagonists.
Journal of medicinal chemistry.
2016 12; 59(24):11050-11068. doi:
10.1021/acs.jmedchem.6b01247. [PMID: 27736063] - Melek Karaca, Rinku Dutta, Yildiz Ozsoy, Ram I Mahato. Micelle Mixtures for Coadministration of Gemcitabine and GDC-0449 To Treat Pancreatic Cancer.
Molecular pharmaceutics.
2016 06; 13(6):1822-32. doi:
10.1021/acs.molpharmaceut.5b00971. [PMID: 26981724] - Chuanqing Wu, Ji Cheng, Shaobo Hu, Rui Deng, Yamba Willy Muangu, Liang Shi, Ke Wu, Peng Zhang, Weilong Chang, Guobin Wang, Kaixiong Tao. Reduced proliferation and increased apoptosis of the SGC‑7901 gastric cancer cell line on exposure to GDC‑0449.
Molecular medicine reports.
2016 Feb; 13(2):1434-40. doi:
10.3892/mmr.2015.4677. [PMID: 26676867] - Wanyun Zhao, Xiaoqi Pan, Tao Li, Changchun Zhang, Nian Shi. Lycium barbarum Polysaccharides Protect against Trimethyltin Chloride-Induced Apoptosis via Sonic Hedgehog and PI3K/Akt Signaling Pathways in Mouse Neuro-2a Cells.
Oxidative medicine and cellular longevity.
2016; 2016(?):9826726. doi:
10.1155/2016/9826726. [PMID: 27143997] - Daniel V T Catenacci, Melissa R Junttila, Theodore Karrison, Nathan Bahary, Margit N Horiba, Sreenivasa R Nattam, Robert Marsh, James Wallace, Mark Kozloff, Lakshmi Rajdev, Deirdre Cohen, James Wade, Bethany Sleckman, Heinz-Josef Lenz, Patrick Stiff, Pankaj Kumar, Peng Xu, Les Henderson, Naoko Takebe, Ravi Salgia, Xi Wang, Walter M Stadler, Frederic J de Sauvage, Hedy L Kindler. Randomized Phase Ib/II Study of Gemcitabine Plus Placebo or Vismodegib, a Hedgehog Pathway Inhibitor, in Patients With Metastatic Pancreatic Cancer.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
2015 Dec; 33(36):4284-92. doi:
10.1200/jco.2015.62.8719. [PMID: 26527777] - Hiromi Mizuochi, Katsunori Fujii, Tadashi Shiohama, Hideki Uchikawa, Naoki Shimojo. Hedgehog signaling is synergistically enhanced by nutritional deprivation and ligand stimulation in human fibroblasts of Gorlin syndrome.
Biochemical and biophysical research communications.
2015 Feb; 457(3):318-23. doi:
10.1016/j.bbrc.2014.12.108. [PMID: 25576868] - Amar Gajjar, Clinton F Stewart, David W Ellison, Sue Kaste, Larry E Kun, Roger J Packer, Stewart Goldman, Murali Chintagumpala, Dana Wallace, Naoko Takebe, James M Boyett, Richard J Gilbertson, Tom Curran. Phase I study of vismodegib in children with recurrent or refractory medulloblastoma: a pediatric brain tumor consortium study.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2013 Nov; 19(22):6305-12. doi:
10.1158/1078-0432.ccr-13-1425. [PMID: 24077351] - Stephen L Garland. Are GPCRs still a source of new targets?.
Journal of biomolecular screening.
2013 Oct; 18(9):947-66. doi:
10.1177/1087057113498418. [PMID: 23945874] - Manish R Sharma, Theodore G Karrison, Bethany Kell, Kehua Wu, Michelle Turcich, David Geary, Soonmo P Kang, Naoko Takebe, Richard A Graham, Michael L Maitland, Richard L Schilsky, Mark J Ratain, Ezra E W Cohen. Evaluation of food effect on pharmacokinetics of vismodegib in advanced solid tumor patients.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2013 Jun; 19(11):3059-67. doi:
10.1158/1078-0432.ccr-12-3829. [PMID: 23553850] - Songzhu Michael An, Qiang Peter Ding, Ling-song Li. Stem cell signaling as a target for novel drug discovery: recent progress in the WNT and Hedgehog pathways.
Acta pharmacologica Sinica.
2013 Jun; 34(6):777-83. doi:
10.1038/aps.2013.64. [PMID: 23708555] - Teresa S Hawley, Irene Riz, Wenjing Yang, Yoshiyuki Wakabayashi, Louis Depalma, Young-Tae Chang, Weiqun Peng, Jun Zhu, Robert G Hawley. Identification of an ABCB1 (P-glycoprotein)-positive carfilzomib-resistant myeloma subpopulation by the pluripotent stem cell fluorescent dye CDy1.
American journal of hematology.
2013 Apr; 88(4):265-72. doi:
10.1002/ajh.23387. [PMID: 23475625] - Petra Hirsova, Samar H Ibrahim, Steven F Bronk, Hideo Yagita, Gregory J Gores. Vismodegib suppresses TRAIL-mediated liver injury in a mouse model of nonalcoholic steatohepatitis.
PloS one.
2013; 8(7):e70599. doi:
10.1371/journal.pone.0070599. [PMID: 23894677] - Patricia M LoRusso, Sarina A Piha-Paul, Monica Mita, A Dimitrios Colevas, Vikram Malhi, Dawn Colburn, Ming Yin, Jennifer A Low, Richard A Graham. Co-administration of vismodegib with rosiglitazone or combined oral contraceptive in patients with locally advanced or metastatic solid tumors: a pharmacokinetic assessment of drug-drug interaction potential.
Cancer chemotherapy and pharmacology.
2013 Jan; 71(1):193-202. doi:
10.1007/s00280-012-1996-6. [PMID: 23064958] - Richard A Graham, Cornelis E C A Hop, Marie T Borin, Bert L Lum, Dawn Colburn, Ilsung Chang, Young G Shin, Vikram Malhi, Jennifer A Low, Mark J Dresser. Single and multiple dose intravenous and oral pharmacokinetics of the hedgehog pathway inhibitor vismodegib in healthy female subjects.
British journal of clinical pharmacology.
2012 Nov; 74(5):788-96. doi:
10.1111/j.1365-2125.2012.04281.x. [PMID: 22458643] - Yandong Shi, Ubiratan Moura, Isabelle Opitz, Alex Soltermann, Hubert Rehrauer, Svenja Thies, Walter Weder, Rolf A Stahel, Emanuela Felley-Bosco. Role of hedgehog signaling in malignant pleural mesothelioma.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2012 Sep; 18(17):4646-56. doi:
10.1158/1078-0432.ccr-12-0599. [PMID: 22733539] - Pietro Ferruzzi, Federica Mennillo, Antonella De Rosa, Cinzia Giordano, Marco Rossi, Giovanni Benedetti, Roberta Magrini, Gal la Pericot Mohr, Vincenzo Miragliotta, Letizia Magnoni, Elisa Mori, Russell Thomas, Patrizia Tunici, Annette Bakker. In vitro and in vivo characterization of a novel Hedgehog signaling antagonist in human glioblastoma cell lines.
International journal of cancer.
2012 Jul; 131(2):E33-44. doi:
10.1002/ijc.27349. [PMID: 22072503] - Jianmei Wu, Patricia M Lorusso, Larry H Matherly, Jing Li. Implications of plasma protein binding for pharmacokinetics and pharmacodynamics of the γ-secretase inhibitor RO4929097.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2012 Apr; 18(7):2066-79. doi:
10.1158/1078-0432.ccr-11-2684. [PMID: 22351688] - Patricia M Lorusso, Antonio Jimeno, Grace Dy, Alex Adjei, Jordan Berlin, Lawrence Leichman, Jennifer A Low, Dawn Colburn, Ilsung Chang, Sravanthi Cheeti, Jin Y Jin, Richard A Graham. Pharmacokinetic dose-scheduling study of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2011 Sep; 17(17):5774-82. doi:
10.1158/1078-0432.ccr-11-0972. [PMID: 21753154] - Richard A Graham, Bert L Lum, Glenn Morrison, Ilsung Chang, Karin Jorga, Brian Dean, Young G Shin, Qin Yue, Teresa Mulder, Vikram Malhi, Minli Xie, Jennifer A Low, Cornelis E C A Hop. A single dose mass balance study of the Hedgehog pathway inhibitor vismodegib (GDC-0449) in humans using accelerator mass spectrometry.
Drug metabolism and disposition: the biological fate of chemicals.
2011 Aug; 39(8):1460-7. doi:
10.1124/dmd.111.039339. [PMID: 21602311] - Harvey Wong, Bruno Alicke, Kristina A West, Patricia Pacheco, Hank La, Tom Januario, Robert L Yauch, Frederic J de Sauvage, Stephen E Gould. Pharmacokinetic-pharmacodynamic analysis of vismodegib in preclinical models of mutational and ligand-dependent Hedgehog pathway activation.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2011 Jul; 17(14):4682-92. doi:
10.1158/1078-0432.ccr-11-0975. [PMID: 21610148] - Yuzhong Deng, Harvey Wong, Richard A Graham, Wenbin Liu, Heuy-shin Shen, Yao Shi, Laixin Wang, Min Meng, Vikram Malhi, Xiao Ding, Brian Dean. Determination of unbound vismodegib (GDC-0449) concentration in human plasma using rapid equilibrium dialysis followed by solid phase extraction and high-performance liquid chromatography coupled to mass spectrometry.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2011 Jul; 879(22):2119-26. doi:
10.1016/j.jchromb.2011.05.048. [PMID: 21704573] - Qin Yue, Yung-Hsiang Chen, Teresa Mulder, Alan Deese, Ryan Takahashi, Patrick J Rudewicz, Mark Reynolds, Eric Solon, Cornelis E C A Hop, Harvey Wong, S Cyrus Khojasteh. Absorption, distribution, metabolism, and excretion of [¹⁴C]GDC-0449 (vismodegib), an orally active hedgehog pathway inhibitor, in rats and dogs: a unique metabolic pathway via pyridine ring opening.
Drug metabolism and disposition: the biological fate of chemicals.
2011 Jun; 39(6):952-65. doi:
10.1124/dmd.110.037374. [PMID: 21363998] - Anthony M Giannetti, Harvey Wong, Gerrit J P Dijkgraaf, Erin C Dueber, Daniel F Ortwine, Brandon J Bravo, Stephen E Gould, Emile G Plise, Bert L Lum, Vikram Malhi, Richard A Graham. Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449).
Journal of medicinal chemistry.
2011 Apr; 54(8):2592-601. doi:
10.1021/jm1008924. [PMID: 21438527] - Richard A Graham, Bert L Lum, Sravanthi Cheeti, Jin Yan Jin, Karin Jorga, Daniel D Von Hoff, Charles M Rudin, Josina C Reddy, Jennifer A Low, Patricia M Lorusso. Pharmacokinetics of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors: the role of alpha-1-acid glycoprotein binding.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2011 Apr; 17(8):2512-20. doi:
10.1158/1078-0432.ccr-10-2736. [PMID: 21300760] - Patricia M LoRusso, Charles M Rudin, Josina C Reddy, Raoul Tibes, Glen J Weiss, Mitesh J Borad, Christine L Hann, Julie R Brahmer, Ilsung Chang, Walter C Darbonne, Richard A Graham, Kenn L Zerivitz, Jennifer A Low, Daniel D Von Hoff. Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2011 Apr; 17(8):2502-11. doi:
10.1158/1078-0432.ccr-10-2745. [PMID: 21300762] - Harvey Wong, Frank-Peter Theil, Yong Cui, James C Marsters, S Cyrus Khojasteh, Laurent Vernillet, Hank La, Xiling Song, Hong Wang, Eric J Morinello, Yuzhong Deng, Cornelis E C A Hop. Interplay of dissolution, solubility, and nonsink permeation determines the oral absorption of the Hedgehog pathway inhibitor GDC-0449 in dogs: an investigation using preclinical studies and physiologically based pharmacokinetic modeling.
Drug metabolism and disposition: the biological fate of chemicals.
2010 Jul; 38(7):1029-38. doi:
10.1124/dmd.110.032680. [PMID: 20406853] - X Ding, B Chou, R A Graham, S Cheeti, S Percey, L C Matassa, S A Reuschel, M Meng, S Liu, T Voelker, B L Lum, P J Rudewicz, C E C A Hop. Determination of GDC-0449, a small-molecule inhibitor of the Hedgehog signaling pathway, in human plasma by solid phase extraction-liquid chromatographic-tandem mass spectrometry.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2010 Mar; 878(9-10):785-90. doi:
10.1016/j.jchromb.2010.01.039. [PMID: 20172765] - H Wong, J Z Chen, B Chou, J S Halladay, J R Kenny, H La, J C Marsters, E Plise, P J Rudewicz, K Robarge, Y Shin, S Wong, C Zhang, S C Khojasteh. Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.
Xenobiotica; the fate of foreign compounds in biological systems.
2009 Nov; 39(11):850-61. doi:
10.3109/00498250903180289. [PMID: 19845436] - Cynthia M Rominger, Wei-Lin Tiger Bee, Robert A Copeland, Elizabeth A Davenport, Aidan Gilmartin, Richard Gontarek, Keith R Hornberger, Lorena A Kallal, Zhihong Lai, Kenneth Lawrie, Quinn Lu, Lynette McMillan, Maggie Truong, Peter J Tummino, Brandon Turunen, Matthew Will, William J Zuercher, David H Rominger. Evidence for allosteric interactions of antagonist binding to the smoothened receptor.
The Journal of pharmacology and experimental therapeutics.
2009 Jun; 329(3):995-1005. doi:
10.1124/jpet.109.152090. [PMID: 19304771] - Yimao Zhang, John Laterra, Martin G Pomper. Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp.
Neoplasia (New York, N.Y.).
2009 Jan; 11(1):96-101. doi:
10.1593/neo.81264. [PMID: 19107236]