Posters and Presentations
Tipifarnib
Preliminary results from a phase 2 trial of tipifarnib in Head and Neck Squamous Cell Carcinomas (HNSCCs) with HRAS mutations
AACR-NCI-EORTC 2019 Presentation
AACR-NCI-EORTC 2019 Poster
Tipifarnib in Relapsed or Refractory Angioimmunoblastic T-cell Lymphoma (AITL) and CXCL12+ Peripheral T-cell Lymphoma (PTCL): Preliminary Results from an Open-Label, Phase 2 Study
ICML 2019 Presentation
KIR3DL2 Mutation may define a high rate of response of AITL to Tipifarnib
ICML 2019 Poster
Tipifarnib in Relapsed or Refractory Angioimmunoblastic T-cell Lymphoma (AITL) and CXCL12+ Peripheral T-cell Lymphoma (PTCL): Preliminary Results from an Open-Label, Phase 2 Study
EHA 2019 Presentation
CXCL12 and CXCR3 may identify complete response in Acute Myeloid Leukemia patients treated with Tipifarnib
EHA 2019 Poster
Mechanism of Action of the Farnesyltransferase Inhibitor Tipifarnib and its Potential Clinical Applications
AACR 2019 Poster
Patient reported abdominal pain as a surrogate of the clinical benefit of tipifarnib in pancreatic cancer patients
ASCO GI 2019 Poster
Tipifarnib in Relapsed or Refractory Angioimmunoblastic T-cell Lymphoma (AITL) and CXCL12+ Peripheral T-cell Lymphoma (PTCL): Preliminary Results from an Open-Label, Phase 2 Study
ASH 2018 Poster
Identification of Tipifarnib Sensitivity Biomarkers in T-Cell Tumor cell lines
ASH 2018 Poster
Tipifarnib is Highly Active in HRAS-mutant Head and Neck Squamous Cell Carcinoma (HNSCC) Tumor Models
EORTC-NCI-AACR 2018 Poster
Preliminary results from a Phase 2 proof of concept trial of tipifarnib in Squamous Cell Carcinomas (SCCs) with HRAS mutations
ESMO 2018 Presentation
Tipifarnib is Highly Active in HRAS-mutant Lung Squamous Cell Carcinoma Tumor Models
AACR 2018 Poster
Pre-clinical Activity of Tipifarnib in Cutaneous T-cell Lymphoma
AACR 2018 Poster
Preliminary Results from a Phase 2 Trial of Tipifarnib in HRAS mutant Head & Neck Squamous Cell Carcinomas (HNSCC)
H&N 2018 Poster
The CXCL12/CXCR4 Pathway As a Potential Target of Tipifarnib in Acute Myeloid Leukemia and Myelodysplastic Syndromes
ASH 2017 Poster
The CXCL12/CXCR4 Pathway As a Potential Target of Tipifarnib: Preliminary Results from an Open-Label, Phase II Study in Relapsed or Refractory Peripheral T-Cell Lymphoma
ASH 2017 Poster
Preliminary results from an open-label, phase 2 study of tipifarnib in chronic myelomonocytic leukemia (CMML)
ASH 2017 Poster
Killer Immunoglobulin-like Receptors (KIR) in Low-Risk Myelodysplastic Syndrome: Genotyping and Gene Expression Evaluation
ASH 2017 Poster
Preliminary results from a phase 2 proof of concept trial of Tipifarnib in tumors with HRAS mutations.
AACR-NCI-EORTC 2017 Presentation
Preliminary results from a phase 2 proof of concept trial of Tipifarnib in tumors with HRAS Mutations.
AACR-NCI-EORTC 2017 Poster
Preliminary results from an open-label, phase II study of tipifarnib in relapsed or refractory peripheral T-cell lymphoma.
EHA 2017 Poster
Preliminary results from an open-label, phase II study of tipifarnib in relapsed or refractory peripheral T-cell lymphoma.
ICML 2017 Poster
Tipifarnib is Highly Active in HRAS-mutant SCCHN Tumor Models.
AACR Head and Neck 2017 Poster
Preliminary evidence of clinical activity with tipifarnib in squamous cell carcinomas of the head & neck (SCCHN) with HRAS mutations.
15th International Congress on Targeted Anticancer Therapies (TAT 2017) Presentation
Targeting the RAS-ERK Pathway.
9th European Scientific Oncology Conference (ESOC-9) Presentation
KO-947 / ERK
11q13 amplification selects for sensitivity to the ERK inhibitor KO-947 in squamous cell carcinomas
AACR 2018 Poster
KO-947, a potent ERK inhibitor with robust preclinical single agent activity in MAPK pathway dysregulated tumors.
AACR 2017 Poster
KO-947, a Potent and Selective ERK Inhibitor with Slow Dissociation Kinetics.
EORTC 2016 Poster
Targeting the RAS-ERK Pathway.
9th European Scientific Oncology Conference (ESOC-9) 2016 Presentation
KO-539 / Menin-MLL
A Novel Small Molecule Menin-MLL Inhibitor for Potential Treatment of MLL-rearranged Leukemias and NPM1/DNMT3A-mutant AML.
AACR-EORTC-NCI 2017 Poster
A Novel Small Molecule Menin-MLL Inhibitor for Potential Treatment of MLL-rearranged Leukemias.
AACR 2017 Poster
Discovery of novel menin-MLL small molecule inhibitors that display high potency and selectivity in vitro and in vivo.
EORTC 2016 Poster
Publications
Tipifarnib
Protein farnesylation:
Cox, et al. Targeting RAS Membrane Association: Back to the Future for Anti-RAS Drug Discovery? Clin. Cancer Res, 21(8), 1819-1827 (April 2015)
Publication
Berndt, et al. Targeting protein prenylation for cancer therapy. Nature Reviews Cancer 11, 775-791 (November 2011)
Publication
HRAS:
Chen, et al. Transformation by Hras(G12V) is consistently associated with mutant allele copy gains and is reversed by farnesyl transferase inhibition. Oncogene, 33(47):5442-9 (2014 Nov 20)
Publication
PTCL:
Witzig, et al. Multi-institutional phase 2 study of the farnesyltransferase inhibitor tipifarnib (R115777) in patients with relapsed and refractory lymphomas. Blood. 2011 Nov 3; 118(18):4882-9
Publication
MDS:
Ghobrial, et al. The bone-marrow niche in MDS and MGUS: implications for AML and MM. Nature Reviews Clinical Oncology. 2018 Jan 9; 15, 219-233
Publication
Fenaux, et al. A multicenter phase 2 study of the farnesyltransferase inhibitor tipifarnib in intermediate- to high-risk myelodysplastic syndrome. Blood. 2007 May 15; 109(10):4158-63
Publication
CMML:
Fenaux, et al. A multicenter phase 2 study of the farnesyltransferase inhibitor tipifarnib in intermediate- to high-risk myelodysplastic syndrome. Blood. 2007 May 15; 109(10):4158-63
Publication
KO-947 / ERK
Samatar and Poulikakos. Targeting RAS–ERK signalling in cancer: promises and challenges. Nature Reviews Drug Discovery 13, 928–942 (2014)
Publication
KO-539 / Menin-MLL
Borkin, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27 (4):589-602
Publication