Therapy Detail

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Therapy Name Tipifarnib
Synonyms
Therapy Description

Zarnestra (tipifarnib) is a farnesyltransferase inhibitor, which alters post-translational modification and activation of Ras proteins, and may result in decreased tumor cell proliferation and reduced tumor growth (PMID: 11196150, PMID: 25323927).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Tipifarnib Zarnestra|R115777 Farnesyltransferase Inhibitor 3 Zarnestra (tipifarnib) is a farnesyltransferase inhibitor, which alters post-translational modification and activation of Ras proteins, and may result in decreased tumor cell proliferation and reduced tumor growth (PMID: 11196150, PMID: 25323927, PMID: 32557577).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
HRAS mutant transitional cell carcinoma predicted - sensitive Tipifarnib Phase II Actionable In a Phase II trial (IST-01), Zarnestra (tipifarnib) treatment resulted in an objective response in 42% (5/12) of patients with urothelial carcinoma harboring HRAS mutations, with a median progression-free survival of 5.1 months (J Clin Oncol 38: 2020 (suppl; abstr 6504); NCT02535650). detail...
HRAS mutant salivary gland cancer predicted - sensitive Tipifarnib Phase II Actionable In a Phase II trial (KO-TIP-001), Zarnestra (tipifarnib) treatment resulted in an objective response rate of 8% (1/12) in patients with recurrent or metastatic salivary gland cancer harboring HRAS mutations, with a median progression-free survival of 7 months (J Clin Oncol 38: 2020 (suppl; abstr 6504); NCT02383927). detail...
HRAS over exp head and neck squamous cell carcinoma predicted - sensitive Tipifarnib Preclinical - Pdx Actionable In a preclinical study, Zarnestra (tipifarnib) treatment resulted in tumor regression in patient-derived xenograft (PDX) models of head and neck squamous cell carcinoma overexpressing wild-type Hras (J Clin Oncol 38: 2020 (suppl; abstr e15658)). detail...
HRAS mutant head and neck squamous cell carcinoma predicted - sensitive Tipifarnib Phase II Actionable In a Phase II trial (KO-TIP-001), Zarnestra (tipifarnib) treatment resulted in an objective response rate of 56% (10/18) in patients with head and neck squamous cell carcinoma harboring HRAS missense mutations at a variant allele frequency over 20%, with a median progression-free survival of 6.1 months (J Clin Oncol 38: 2020 (suppl; abstr 6504); NCT02383927). detail...
HRAS act mut transitional cell carcinoma predicted - sensitive Tipifarnib Phase II Actionable In a Phase II trial, Zarnestra (tipifarnib) demonstrated safety and preliminary efficacy in patients with metastatic urothelial carcinoma harboring HRAS mutations (n=14) or STK11:rs2075606, 3 of 4 patients achieved progression-free survival at 6 months harbored HRAS activating mutations, and no response was observed in HRAS wild-type patients (J Clin Oncol 38: 2020 (suppl; abstr 5086); NCT02535650). detail...
HRAS mutant salivary gland carcinoma sensitive Tipifarnib Clinical Study Actionable In a clinical study, Zarnestra (tipifarnib) treatment resulted in an overall response rate of 8% (n=13) with one ongoing partial response with a duration of 14 months and stable disease as the best response in 58% (7/12) of evaluable patients with HRAS-mutant metastatic salivary gland carcinoma, and a median overall survival of 18 months, and a median progression-free survival of 7 months (PMID: 32557577). 32557577

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Clinical Trial Phase Therapies Title Recruitment Status
NCT02807272 Phase II Tipifarnib Tipifarnib in Subjects With Chronic Myelomonocytic Leukemia (CMML) Active, not recruiting
NCT00006199 Phase I Tipifarnib Topotecan Study of the Farnesyl Transferase Inhibitor, R115777, in Combination With Topotecan (NYU 99-32) Unknown status
NCT02464228 Phase II Tipifarnib Study of Tipifarnib in Subjects With Relapsed or Refractory Peripheral T-Cell Lymphoma Active, not recruiting
NCT02383927 Phase II Tipifarnib Phase II Study of Tipifarnib in Squamous Head and Neck Cancer With HRAS Mutations Active, not recruiting
NCT03719690 Phase II Tipifarnib Safety and Efficacy of Tipifarnib in Head and Neck Cancer With HRAS Mutations and Impact of HRAS on Response to Therapy (AIM-HN/SEQ-HN) Recruiting
NCT02779777 Phase II Tipifarnib Tipifarnib in Subjects With Transfusion-dependent, Very Low, Low, or Intermediate Risk Myelodysplastic Syndromes Terminated
NCT04284774 Phase II Tipifarnib Tipifarnib for the Treatment of Advanced Solid Tumors, Lymphoma, or Histiocytic Disorders With HRAS Gene Alterations, a Pediatric MATCH Treatment Trial Recruiting


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