Drugs / tipifarnib
last change Aug 2025 re-read 2 minutes ago

tipifarnib

also known as R115777 · Zarnestra · NSC 702818 · NSC #70818 · R11577 · R15777

Small molecule targets HRAS via inhibition

Developed for
acute myeloid leukemia, t(16;16)(p13.1;q22) · acute megakaryoblastic leukemia in adult · acute myeloblastic leukemia with maturation · acute myeloblastic leukemia without maturation · acute myeloid leukemia with minimal differentiation · acute myeloid leukemia, inv(16)(p13.1;q22) · acute myelomonocytic leukemia M4 · adult acute monocytic leukemia
+108 more · acute myeloid leukemia with t(8;21)(q22;q22) translocation · acute myeloid leukemia with 11q23 abnormalities · leukemia · acute myeloid leukemia, del(5q31-q32) · erythroleukemia · female breast carcinoma · myelodysplastic syndrome · acute erythroid leukemia · acute myeloid leukemia · adult glioblastoma · chronic myelomonocytic leukemia · giant cell glioblastoma · gliosarcoma · plasma cell myeloma · acute basophilic leukemia · acute myeloid leukemia with multilineage dysplasia · breast cancer · cancer · cancer of unknown primary site · head and neck squamous cell carcinoma · malignant pancreatic neoplasm · myelodysplastic syndrome with excess blasts · neuroblastoma · non-small cell lung carcinoma · acute myeloid leukemia and myelodysplastic syndromes related to alkylating agent · acute myeloid leukemia with t(9;11)(p22;q23) · acute myeloid leukemia, t(8;21)(q22; q22.1) · childhood brain stem glioma · ependymoma · Ewing sarcoma · glioblastoma · hepatoblastoma · inflammatory breast carcinoma · Langerhans cell histiocytosis · male breast carcinoma · malignant germ cell tumor · malignant glioma · mantle cell lymphoma · medulloblastoma · melanoma · neoplasm · non-Hodgkin lymphoma · peripheral primitive neuroectodermal tumor · refractory anemia with excess blasts in transformation · rhabdomyosarcoma · therapy related acute myeloid leukemia and myelodysplastic syndrome · acquired polycythemia vera · acute myeloid leukemia with abnormal bone marrow eosinophils inv(16)(p13q22) or t(16;16)(p13;q22) · acute myeloid leukemia, t(9;11)(p21.3;q23.3) · acute promyelocytic leukemia · adrenal gland pheochromocytoma · adult acute lymphoblastic leukemia · adult T-cell leukemia/lymphoma · anaplastic large cell lymphoma · atypical chronic myeloid leukemia, BCR-ABL1 negative · bladder transitional cell carcinoma · breast neoplasm · central nervous system neoplasm · childhood cerebellar astrocytic neoplasm · childhood cerebral astrocytoma · childhood medulloblastoma · childhood myelodysplastic syndrome · childhood oligodendroglioma · chronic lymphocytic leukemia/small lymphocytic lymphoma · chronic myeloid leukemia · colorectal cancer · conventional osteosarcoma · ectomesenchymoma · essential thrombocythemia · estrogen-receptor positive breast cancer · histiocytic sarcoma · Hodgkins lymphoma · juvenile myelomonocytic leukemia · juvenile xanthogranuloma · kidney Wilms tumor · leukemia, myeloid, accelerated-phase · lung cancer · lung carcinoma · MALT lymphoma · mature T-cell and NK-cell non-Hodgkin lymphoma · metastatic melanoma · myelodysplastic syndrome with multilineage dysplasia · myelodysplastic syndrome with ring sideroblasts · myeloproliferative neoplasm · myeloproliferative neoplasm, unclassifiable · neurofibromatosis type 1 · nodal marginal zone B-cell lymphoma · optic pathway glioma · osteosarcoma · pancreatic adenocarcinoma · pancreatic neoplasm · plasma cell neoplasm · plexiform neurofibroma · primary myelofibrosis · primary organ-specific lymphoma · prostate cancer · renal pelvis/ureter urothelial carcinoma · rhabdoid tumor · rhabdoid tumor of the kidney · small cell lung carcinoma · splenic marginal zone lymphoma · supratentorial primitive neuroectodermal tumor · T-cell large granular lymphocyte leukemia · thyroid cancer · thyroid gland carcinoma · urinary bladder cancer · urothelial carcinoma · Wilms tumor
Investigated by
National Cancer Institute (NCI) · Kura Oncology, Inc. · Johnson & Johnson Pharmaceutical Research & Development, L.L.C. · H. Lee Moffitt Cancer Center and Research Institute · Janssen-Cilag Ltd. · Abramson Cancer Center at Penn Medicine
+27 more · Institut Claudius Regaud · M.D. Anderson Cancer Center · Millennium Pharmaceuticals, Inc. · NYU Langone Health · SWOG Cancer Research Network · The University of Texas Health Science Center at San Antonio · University Health Network, Toronto · Children's Oncology Group · City of Hope Medical Center · Emory University · Fox Chase Cancer Center · Giselle Sholler · Johnson & Johnson · Lymphoma Study Association · Mayo Clinic · NRG Oncology · National Center for Research Resources (NCRR) · National Institutes of Health (NIH) · National Institutes of Health Clinical Center (CC) · Ohio State University Comprehensive Cancer Center · Ortho Biotech, Inc. · Samsung Medical Center · Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins · Spanish Lung Cancer Group · The University of New South Wales · University of Bologna · University of Maryland, Baltimore

Trials 88 · started per year

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PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 124 trials
Phase 1 NCT05693090 Feb 2023 → Jul 2027 non-small cell lung carcinoma Kura Oncology, Inc. Withdrawn No outcome recorded
Phase 1 NCT04865159 May 2021 → May 2023 neoplasm Kura Oncology, Inc. Terminated No outcome recorded
Phase 1 NCT00101153 Apr 2007 → Mar 2010 leukemia University Health Network, Toronto Completed No outcome recorded
Phase 1 NCT00972712 Dec 2006 → Dec 2009 plasma cell myeloma Emory University Completed No outcome recorded
Phase 1 NCT00383474 Aug 2006 → Jun 2012 acute basophilic leukemia, acute megakaryoblastic leukemia in adult, acute myeloblastic leukemia with maturation, acute myeloblastic leukemia without maturation +9 National Cancer Institute (NCI) Completed No outcome recorded
Phase 1 NCT00124644 Mar 2006 → Dec 2007 leukemia Ohio State University Comprehensive Cancer Center Terminated No outcome recorded
Phase 1 NCT00244972 Oct 2005 → Mar 2017 cancer National Cancer Institute (NCI) Completed No outcome recorded
Phase 1 NCT00112853 Mar 2005 → May 2009 acute erythroid leukemia, acute megakaryoblastic leukemia in adult, acute myeloblastic leukemia with maturation, acute myeloblastic leukemia without maturation +8 National Cancer Institute (NCI) Completed No outcome recorded
Phase 1 NCT00101296 Oct 2004 → May 2011 acute erythroid leukemia, acute megakaryoblastic leukemia in adult, acute myeloblastic leukemia with maturation, acute myeloblastic leukemia without maturation +9 National Cancer Institute (NCI) Completed No outcome recorded
Phase 1 NCT00085553 May 2004 → May 2008 neoplasm National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/212 trials
Phase 1/2 NCT04997902 Dec 2021 → Aug 2025 head and neck squamous cell carcinoma Kura Oncology, Inc. Completed No outcome recorded
Phase 1/2 NCT00470301 Apr 2007 → Sep 2013 male breast carcinoma National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/2 NCT00335764 Apr 2006 → Feb 2010 adult glioblastoma, giant cell glioblastoma, gliosarcoma National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/2 NCT00100750 Sep 2005 → Oct 2007 female breast carcinoma National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/2 NCT00243035 Aug 2005 → Feb 2007 plasma cell myeloma National Cancer Institute (NCI) Terminated No outcome recorded
Phase 1/2 NCT00361088 Aug 2005 → Jun 2007 plasma cell myeloma H. Lee Moffitt Cancer Center and Research Institute Terminated No outcome recorded
Phase 1/2 NCT00096122 Sep 2004 → Sep 2006 acute basophilic leukemia, acute megakaryoblastic leukemia in adult, acute myeloblastic leukemia with maturation, acute myeloblastic leukemia without maturation +12 National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/2 NCT00079339 Jan 2004 → Nov 2009 childhood brain stem glioma National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/2 NCT00070252 Sep 2003 → Feb 2006 female breast carcinoma, inflammatory breast carcinoma, male breast carcinoma National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/2 NCT00050986 Dec 2002 → Oct 2008 glioblastoma M.D. Anderson Cancer Center Completed No outcome recorded
Phase 248 trials
Phase 2 NCT06540963 Dec 2024 → Dec 2030 expected neuroblastoma Giselle Sholler Recruiting No outcome recorded
Phase 2 NCT04284774 Oct 2020 → Mar 2024 overdue Ewing sarcoma, Langerhans cell histiocytosis, adrenal gland pheochromocytoma, ectomesenchymoma +14 National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 2 NCT03719690 Mar 2019 → May 2023 head and neck squamous cell carcinoma Kura Oncology, Inc. Completed No outcome recorded
Phase 2 NCT03496766 May 2018 → Oct 2022 non-small cell lung carcinoma Spanish Lung Cancer Group Terminated No outcome recorded
Phase 2 NCT03155620 Jul 2017 → Mar 2025 overdue Ewing sarcoma, Langerhans cell histiocytosis, Wilms tumor, conventional osteosarcoma +13 National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 2 NCT02807272 Jan 2017 → Nov 2020 chronic myelomonocytic leukemia Kura Oncology, Inc. Completed No outcome recorded
Phase 2 NCT02779777 Jun 2016 → Aug 2018 myelodysplastic syndrome Kura Oncology, Inc. Terminated No outcome recorded
Phase 2 NCT02464228 Feb 2016 → Mar 2021 mature T-cell and NK-cell non-Hodgkin lymphoma Kura Oncology, Inc. Completed No outcome recorded
Phase 2 NCT02535650 Nov 2015 → Mar 2022 urothelial carcinoma Samsung Medical Center Unknown No outcome recorded
Phase 2 NCT02383927 May 2015 → Dec 2020 head and neck squamous cell carcinoma, thyroid cancer Kura Oncology, Inc. Completed No outcome recorded
Phase 2/31 trial
Phase 2/3 NCT00454480 Aug 2006 → Aug 2012 leukemia, myelodysplastic syndrome The University of New South Wales Completed No outcome recorded
Phase 33 trials
Phase 3 NCT00093470 Aug 2004 → Feb 2015 acute megakaryoblastic leukemia in adult, acute myeloblastic leukemia with maturation, acute myeloblastic leukemia without maturation, acute myeloid leukemia and myelodysplastic syndromes related to alkylating agent +9 National Cancer Institute (NCI) Completed No outcome recorded
Phase 3 NCT00093990 Jan 2004 → Oct 2007 acute myeloid leukemia Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Completed No outcome recorded
Phase 3 NCT00005648 Nov 1999 → Nov 2003 pancreatic neoplasm Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Completed No outcome recorded
Also used as a comparator or background therapy in 1 trial
PhaseRegistry idDatesIndicationSponsorStatusOutcome
NCT04809233 Background peripheral T-cell lymphoma, not otherwise specified Kura Oncology, Inc. Available No outcome recorded

Evidence & citations 11 cited values

Every value below carries the sentence it was read from. 96 sources stand behind the page.

FieldValueCited text
Known as tipifarnib “gemcitabine with and without tipifarnib (referred to as R115777).” NCT00005648
79

NCT00005967

NCT00005041

NCT00058097

NCT00077363

NCT00005845

NCT00005842

NCT00244972

NCT00005848

NCT00048503

NCT02227901

NCT00006376

NCT00077519

NCT00093990

NCT05693090

NCT00101296

NCT00360776

NCT00026104

NCT06540963

NCT00025480

NCT04809233

NCT00022451

NCT00082810

NCT00049114

NCT00847223

NCT00045396

NCT00049387

NCT00082888

NCT00383474

NCT02210858

NCT04284774

NCT00972712

NCT00052728

NCT02779777

NCT00093470

NCT02535650

NCT00454480

NCT00096122

NCT00005843

NCT00079339

NCT00112853

NCT00021541

NCT04865159

NCT00047216

NCT00027872

NCT04997902

NCT00070252

NCT00025038

NCT00085553

NCT02383927

NCT02807272

NCT00470301

NCT00335764

NCT00281957

NCT00004009

NCT00070525

NCT00354146

NCT00602771

NCT00050154

NCT00025454

NCT00093418

NCT00005859

NCT00055757

NCT00101153

NCT00050141

NCT00124644

NCT00243035

NCT00100750

NCT01361464

NCT00510939

NCT00005990

NCT03496766

NCT00005989

NCT00003707

NCT00060125

NCT00047190

NCT00054470

NCT03155620

NCT02464228

NCT03719690

Known as NSC #70818 “Phase II trial of R115777 (NSC #70818) in patients with advanced colorectal” PMID 16683076 Jul 2006
Known as NSC 702818 “Phase II Trial of R115777 (NSC-702818), an Inhibitor of Farnesyl Protein Transferase, in Patients With Previously Untreated Metastatic Pancreatic Adenocarcinoma” NCT00005843
1

“Phase I/II Study of Tipifarnib [Zarnestra, Farnesyltransferase Inhibitor R115777 (NSC 702818)] in Patients With Myeloproliferative Disorders” NCT02210858

Known as R11577 ClinicalTrials.gov intervention name — accepted as the source's own label NCT00361088
Known as R115777 “Tipifarnib (R115777) inhibits farnesylation of key proteins that modulate signaling pathways implicated in cell growth and proliferation, including members of the Ras and Rho families.” PMID 15711184 Mar 2005
16

“Phase II Trial of R115777 (NSC-702818), an Inhibitor of Farnesyl Protein Transferase, in Patients With Previously Untreated Metastatic Pancreatic Adenocarcinoma” NCT00005843

“Multi-institutional phase 2 study of the farnesyltransferase inhibitor tipifarnib (R115777) in patients with relapsed and refractory lymphomas.” PMID 21725056 Jul 2011

“A Phase II Study of R115777 (Zarnestra) in Superficial Transitional Cell Carcinoma of Bladder” NCT00047216

“Dose-ranging pharmacodynamic study of tipifarnib (R115777) in patients with” PMID 15570084 Dec 2004

“Patients receive oral R115777 twice daily on days 1-21.” NCT00012350

“ZARNESTRA, tipifarnib, R115777NCT00050154

“ZARNESTRA, tipifarnib, R115777NCT00050141

“ZARNESTRA, tipifarnib, R115777NCT00048503

“Tipifarnib;Zarnestra; R115777NCT00093990

“tipifarnib (R115777)” NCT00354146

“Zarnestra (R115777)” NCT00040105

NCT00050986

NCT00005833

NCT00005832

NCT00005648

NCT00006199

Known as R15777 “A Phase II Trial Of Tipifarnib (R15777, ZARNESTRA) In Combination With Tamoxifen In Subjects With Metastatic Breast Cancer” NCT00052728
Known as Zarnestra “A Phase II Trial Of Tipifarnib (R15777, ZARNESTRA) In Combination With Tamoxifen In Subjects With Metastatic Breast Cancer” NCT00052728
10

“A Phase II Study of R115777 (Zarnestra) in Superficial Transitional Cell Carcinoma of Bladder” NCT00047216

“tipifarnib (ZARNESTRA) treatment” NCT01361464

ZARNESTRA, tipifarnib, R115777” NCT00048503

ZARNESTRA, tipifarnib, R115777” NCT00050154

ZARNESTRA, tipifarnib, R115777” NCT00050141

“Tipifarnib;Zarnestra; R115777” NCT00093990

ZARNESTRA (Tipifarnib)” NCT00847223

NCT00209989

NCT00210028

NCT00040105

Action Inhibit “R115777, an oral farnesyl transferase inhibitor” PMID 16133800 Oct 2005
Modality Small molecule “R115777 is a selective nonpeptidomimetic inhibitor of farnesyltransferase (FTase), one of several enzymes responsible for posttranslational modification that is required for...” PMID 12663718 Apr 2003
Route Oral oral tipifarnib every 12 hours beginning on day 2” NCT00003707
Target HRAS “disrupts HRAS function” PMID 33750196 Mar 2021