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AnneMarie Culazzo Pferdekamper
Researcher at Genomics Institute of the Novartis Research Foundation
Publications - 7
Citations - 1522
AnneMarie Culazzo Pferdekamper is an academic researcher from Genomics Institute of the Novartis Research Foundation. The author has contributed to research in topics: ALK inhibitor & Anaplastic lymphoma kinase. The author has an hindex of 5, co-authored 6 publications receiving 1351 citations.
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Journal ArticleDOI
The ALK Inhibitor Ceritinib Overcomes Crizotinib Resistance in Non–Small Cell Lung Cancer
Luc Friboulet,Nanxin Li,Ryohei Katayama,Christian C. Lee,Justin F. Gainor,Adam S. Crystal,Pierre-Yves Michellys,Mark M. Awad,Noriko Yanagitani,Sungjoon Kim,AnneMarie Culazzo Pferdekamper,Jie Li,Shailaja Kasibhatla,Frank Sun,Xiuying Sun,Su Hua,Peter McNamara,Sidra Mahmood,Elizabeth L. Lockerman,Naoya Fujita,Makoto Nishio,Jennifer L. Harris,Alice T. Shaw,Jeffrey A. Engelman +23 more
TL;DR: The first preclinical evaluation of the next-generation ALK TKI, ceritinib (LDK378), in the setting of crizotinib resistance demonstrates that ceritInib can overcome crizotib resistance, consistent with clinical data showing marked efficacy of cerit inib in patients with crizotonib-resistant disease.
Journal ArticleDOI
Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials
Thomas H. Marsilje,Wei Pei,Bei Chen,Wenshuo Lu,Tetsuo Uno,Jin Yunho,Tao Jiang,Sungjoon Kim,Nanxin Li,Markus Warmuth,Yelena Sarkisova,Frank Sun,Auzon Steffy,AnneMarie Culazzo Pferdekamper,Allen G. Li,Sean B. Joseph,Young Kim,Bo Liu,Tove Tuntland,Xiaoming Cui,Nathanael S. Gray,Ruo Steensma,Yongqin Wan,Jiqing Jiang,Chopiuk Greg,Jie Li,W. Perry Gordon,Wendy Richmond,Kevin Johnson,Jonathan Chang,Todd Groessl,You-Qun He,Andrew Phimister,Alex Aycinena,Christian C. Lee,Badry Bursulaya,Donald S. Karanewsky,H. Martin Seidel,Jennifer L. Harris,Pierre-Yves Michellys +39 more
TL;DR: In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684).
Journal ArticleDOI
Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist
Shifeng Pan,Xu Wu,Jiqing Jiang,Wenqi Gao,Yongqin Wan,Dai Cheng,Dong Han,Jun Liu,Nathan P. Englund,Yan Wang,Stefan Peukert,Karen Miller-Moslin,Jing Yuan,Ribo Guo,Melissa Matsumoto,Anthony Vattay,Yun Jiang,Jeffrey Tsao,Fangxian Sun,AnneMarie Culazzo Pferdekamper,Stephanie Kay Dodd,Tove Tuntland,Wieslawa Maniara,Joseph Kelleher,Yung-mae Yao,Markus Warmuth,Juliet Williams,Marion Dorsch +27 more
TL;DR: Structural-activity relationship studies led to the discovery of a potent and specific Smoothened antagonist N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4'-(trifluoromethoxy)biphenyl- 3-carboxamide (5m, NVP-LDE225), which is currently in clinical development.
Journal ArticleDOI
EGF816 Exerts Anticancer Effects in Non–Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor
Yong Jia,Jose Juarez,Jie Li,Mari Manuia,Matthew J. Niederst,Celin Tompkins,Noelito Timple,Mei-Ting Vaillancourt,AnneMarie Culazzo Pferdekamper,Elizabeth L. Lockerman,Chun Li,Jennifer Anderson,Carlotta Costa,Debbie Liao,Eric Murphy,Michael DiDonato,Badry Bursulaya,Gerald Lelais,Jordi Barretina,Matthew McNeill,Robert Epple,Thomas H. Marsilje,Nuzhat Pathan,Jeffrey A. Engelman,Pierre-Yves Michellys,Peter McNamara,Jennifer L. Harris,Bender Steven Lee,Shailaja Kasibhatla +28 more
TL;DR: The first preclinical characterization of EGF816 is reported, which provides the groundwork for its current evaluation in phase I/II clinical trials in patients harboring EGFR mutations, including T790M.
Proceedings ArticleDOI
Abstract B232: Activity of a potent and selective phase I ALK inhibitor LDK378 in naive and crizotinib-resistant preclinical tumor models.
Nanxin Li,Pierre-Yves Michellys,Sungjoon Kim,AnneMarie Culazzo Pferdekamper,Jie Li,Shailaja Kasibhatla,Celin Tompkins,Auzon Steffy,Allen G. Li,Frank Sun,Xiuying Sun,Su Hua,Ralph Tiedt,Yelena Sarkisova,Thomas H. Marsilje,Peter McNamara,Jennifer L. Harris +16 more
TL;DR: The results from these preclinical studies suggest that LDK378 may be active in crizotinib-relapsed patients and that the drug exposure associated with this dose is predicted to be below the exposure at the MTD in humans.