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Details:

Tipifarnib, a potent and selective farnesyltransferase inhibitor, is being investigated for the treatment of HRAS mutant head and neck squamous cell carcinoma.


Lead Product(s): Tipifarnib

Therapeutic Area: Oncology Product Name: Zarnestra

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 17, 2023

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R115777 (tipifarnib), a potent, selective and orally bioavailable FTI, has received Breakthrough Therapy Designation for the treatment of patients with HRAS mutant HNSCC and is currently in a registration-directed trial (AIM-HN) in patients with this devastating disease.


Lead Product(s): Tipifarnib,Alpelisib

Therapeutic Area: Oncology Product Name: R115777

Highest Development Status: Phase I/ Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 26, 2022

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Preclinical data supporting the potential of its farnesyl transferase inhibitor (FTI) tipifarnib to prevent emergence of resistance to the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor osimertinib in EGFR mutant non-small cell lung cancer (NSCLC).


Lead Product(s): Tipifarnib,Osimertinib Mesylate

Therapeutic Area: Oncology Product Name: Zarnesta

Highest Development Status: PreclinicalProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable April 08, 2022

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Zarnesta (tipifarnib), a potent, selective and orally bioavailable farnesyl transferase inhibitor, is currently in a registration-directed trial (AIM-HN) in patients with this devastating disease.


Lead Product(s): Tipifarnib,Alpelisib

Therapeutic Area: Oncology Product Name: Zarnesta

Highest Development Status: Phase I/ Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 08, 2022

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Combination of tipifarnib, a farnesyl transferase inhibitor with Novartis’ alpelisib, a PI3Kα inhibitor provide greater antitumor activity, relative to inhibiting either target alone. The combination has potential to address up to 50% of patients with HNSCC in KURRENT trial.


Lead Product(s): Tipifarnib,Alpelisib

Therapeutic Area: Oncology Product Name: Zarnesta

Highest Development Status: Phase I/ Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Novartis Pharmaceuticals Corporation

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 16, 2021

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Tipifarnib was generally well-tolerated in this Phase 2 study, with adverse events consistent with its known safety profile. The most frequently observed treatment-related adverse events (all grades) were hematological and gastrointestinal, as well as fatigue.


Lead Product(s): Tipifarnib

Therapeutic Area: Oncology Product Name: Zarnesta

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable December 13, 2021

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Tipifarnib is currently being evaluated in an ongoing registration-directed clinical trial (AIM-HN) in this indication of high unmet need.


Lead Product(s): Tipifarnib

Therapeutic Area: Oncology Product Name: Zarnesta

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable February 24, 2021

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Company’s late-stage drug candidate, tipifarnib, shows compelling activity when combined with a PI3Kα inhibitor in models of HRAS/PI3K-dysregulated H&N squamous cell carcinoma, including tumors with PIK3CA mutations or amplifications as well as HRAS overexpression.


Lead Product(s): Tipifarnib,PI3Kα-targeted therapy

Therapeutic Area: Oncology Product Name: Undisclosed

Highest Development Status: PreclinicalProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 26, 2020

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Oral presentation to highlight clinical data for tipifarnib in HRAS mutant solid tumors, including overall survival data in head and neck squamous cell carcinoma.


Lead Product(s): Tipifarnib

Therapeutic Area: Oncology Product Name: Undisclosed

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable May 13, 2020

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Company plans to initiate a registration-directed trial of tipifarnib in advanced nodal lymphomas of TFH phenotype, including AITL, in second half of 2020.


Lead Product(s): Tipifarnib

Therapeutic Area: Oncology Product Name: Undisclosed

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 03, 2020

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