TIPIFARNIB

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C27H22Cl2N4O
Molecular Weight	489.396
Optical Activity	( + )
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1C=NC=C1[C@@](N)(C2=CC=C(Cl)C=C2)C3=CC4=C(C=C3)N(C)C(=O)C=C4C5=CC=CC(Cl)=C5

InChI

InChIKey=PLHJCIYEEKOWNM-HHHXNRCGSA-N

InChI=1S/C27H22Cl2N4O/c1-32-16-31-15-25(32)27(30,18-6-9-20(28)10-7-18)19-8-11-24-23(13-19)22(14-26(34)33(24)2)17-4-3-5-21(29)12-17/h3-16H,30H2,1-2H3/t27-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C27H22Cl2N4O
Molecular Weight	489.396
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.fda.gov/ohrms/dockets/ac/05/briefing/2005-4138B1_01_J&J-Briefing-Document.pdf | https://www.ncbi.nlm.nih.gov/pubmed/11196150

Tipifarnib is an oral farnesyltransferase (FTase) inhibitor which was developed by Janssen (J&J). Upon administration, tipifarnib inhibits FTase and thus suppresses the activity of downstream effectors. The drug reached phase III of clinical trials for such diseases as pancreatic cancer (terminated), colorectal cancer (terminated) and acute myeloid leukemia (in elderly patients).

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Protein farnesyltransferase 13 Target ID: CHEMBL2094108 Sources: http://www.fda.gov/ohrms/dockets/ac/05/briefing/2005-4138b1_01_j&j-briefing-document.pdf	Inhibitor 8504		7.9 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Acute myeloid leukemia 141 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19470696	Primary	Phase III 665	Unknown Approved Use Unknown
Pancreatic cancer 98 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15084616	Primary	Phase III 665	Unknown Approved Use Unknown
Colorectal cancer 102 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15459217	Primary	Phase III 665	Unknown Approved Use Unknown
Peripheral T-cell lymphoma 2 Sources: https://clinicaltrials.gov/ct2/show/NCT02464228	Primary	Phase II 1147	Unknown Approved Use Unknown
Myelodysplastic syndromes 61 Sources: https://clinicaltrials.gov/ct2/show/NCT00045396	Primary	Phase II 1147	Unknown Approved Use Unknown
Chronic myelomonocytic leukemia 5 Sources: https://clinicaltrials.gov/ct2/show/NCT02807272	Primary	Phase II 1147	Unknown Approved Use Unknown
Squamous head and neck cancer with HRAS mutations 1 Sources: https://clinicaltrials.gov/ct2/show/NCT02383927	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
634 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16170172	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		TIPIFARNIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Co-administered	Analyte	Population
3.8 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16170172	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		TIPIFARNIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

T_1/2

Value	Dose	Co-administered	Analyte	Population
3.66 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/16170172	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		TIPIFARNIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.7% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/17268526			TIPIFARNIB plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
200 mg/m2 2 times / day steady, oral MTD Dose: 200 mg/m2, 2 times / day Route: oral Route: steady Dose: 200 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	unhealthy, 4-18 years Health Status: unhealthy Age Group: 4-18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	DLT: Thrombocytopenia, Anemia... Other AEs: Leukopenia, Neutropenia... Dose limiting toxicities: Thrombocytopenia (grade 3, 1 patient) Anemia (grade 4, 1 patient) Other AEs: Leukopenia (grade 2, 1 patient) Neutropenia (grade 2, 1 patient) Lymphopenia (grade 2, 1 patient) Abdominal discomfort (grade 2, 1 patient) Nausea (grade 2, 2 patients) Vomiting (grade 2, 2 patients) Diarrhea (grade 2, 1 patient) Prothrombin time increased (grade 1, 1 patient) Fibrinogen decreased (grade 1, 1 patient) Anorexia (grade 1, 1 patient) Mucositis (grade 1, 1 patient) Gastroesophageal reflux (grade 1, 1 patient) Alkaline phosphatase increased (grade 2, 1 patient) Fatigue (grade 1, 1 patient) Rigor (grade 1, 1 patient) Fever (grade 1, 1 patient) Rash (grade 1, 1 patient) Pruritus (grade 1, 2 patients) Dry skin (grade 2, 1 patient) Muscle contractions involuntary (grade 2, 1 patient) Sensory neuropathy (grade 1, 1 patient) Abnormal gait (grade 2, 1 patient) Triglyceride increased (grade 1, 1 patient) Hypokalemia (grade 1, 1 patient) Pain (grade 1, 2 patients) Rhinitis (grade 1, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16421428
200 mg/m2 2 times / day steady, oral MTD Dose: 200 mg/m2, 2 times / day Route: oral Route: steady Dose: 200 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	unhealthy, 4-18 years Health Status: unhealthy Age Group: 4-18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	DLT: Neutropenia... Dose limiting toxicities: Neutropenia (grade 4, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16421428
200 mg/m2 2 times / day steady, oral Dose: 200 mg/m2, 2 times / day Route: oral Route: steady Dose: 200 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	unhealthy, 4-18 years Health Status: unhealthy Age Group: 4-18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	DLT: Rash... Dose limiting toxicities: Rash (grade 3) Sources: https://pubmed.ncbi.nlm.nih.gov/16421428
275 mg/m2 2 times / day steady, oral Dose: 275 mg/m2, 2 times / day Route: oral Route: steady Dose: 275 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	unhealthy, 4-18 years Health Status: unhealthy Age Group: 4-18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	DLT: Neutropenia, Thrombocytopenia... Dose limiting toxicities: Neutropenia (grade 4, 2 patients) Thrombocytopenia (grade 3, 2 patients) Diarrhea (grade 3, 1 patient) Urinary tract infection (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16421428
375 mg/m2 2 times / day steady, oral Dose: 375 mg/m2, 2 times / day Route: oral Route: steady Dose: 375 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	unhealthy, 4-18 years Health Status: unhealthy Age Group: 4-18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	DLT: Rash, Nausea... Dose limiting toxicities: Rash (grade 3-4, 2 patients) Nausea (grade 3, 1 patient) Vomiting (grade 3, 1 patient) Diarrhea (grade 3, 1 patient) Dehydration (grade 3, 1 patient) Neutropenia (grade 4, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16421428
375 mg/m2 2 times / day steady, oral Dose: 375 mg/m2, 2 times / day Route: oral Route: steady Dose: 375 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	unhealthy, 4-18 years Health Status: unhealthy Age Group: 4-18 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/16421428	DLT: Hypofibrinogenemia... Dose limiting toxicities: Hypofibrinogenemia (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16421428
125 mg/m2 2 times / day steady, oral MTD Dose: 125 mg/m2, 2 times / day Route: oral Route: steady Dose: 125 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18417739	unhealthy, 5.9 years (range: 3.6–13.8 years) Health Status: unhealthy Age Group: 5.9 years (range: 3.6–13.8 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/18417739	DLT: Rash... Dose limiting toxicities: Rash (grade 3) Sources: https://pubmed.ncbi.nlm.nih.gov/18417739
150 mg/m2 2 times / day steady, oral Dose: 150 mg/m2, 2 times / day Route: oral Route: steady Dose: 150 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18417739	unhealthy, 5.9 years (range: 3.6–13.8 years) Health Status: unhealthy Age Group: 5.9 years (range: 3.6–13.8 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/18417739	DLT: Neutropenia, Rash... Dose limiting toxicities: Neutropenia (grade 4) Rash (grade 3) Sources: https://pubmed.ncbi.nlm.nih.gov/18417739
150 mg/m2 2 times / day steady, oral Dose: 150 mg/m2, 2 times / day Route: oral Route: steady Dose: 150 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18417739	unhealthy, 5.9 years (range: 3.6–13.8 years) Health Status: unhealthy Age Group: 5.9 years (range: 3.6–13.8 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/18417739	DLT: Pneumonitis... Dose limiting toxicities: Pneumonitis (grade 3) Sources: https://pubmed.ncbi.nlm.nih.gov/18417739
1600 mg 2 times / day steady, oral Highest studied dose Dose: 1600 mg, 2 times / day Route: oral Route: steady Dose: 1600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/21625235	unhealthy, 61 years (range 33–79 years) Health Status: unhealthy Age Group: 61 years (range 33–79 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/21625235	DLT: Creatinine increased... Dose limiting toxicities: Creatinine increased (grade 2, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/21625235
1200 mg 2 times / day steady, oral MTD Dose: 1200 mg, 2 times / day Route: oral Route: steady Dose: 1200 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/21625235	unhealthy, 61 years (range 33–79 years) Health Status: unhealthy Age Group: 61 years (range 33–79 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/21625235	Other AEs: Creatinine increased, Anorexia... Other AEs: Creatinine increased (grade 3, 1 patient) Anorexia (grade 2, 1 patient) Hyperglycemia (grade 2, 2 patients) Fatigue (grade 2, 3 patients) Alopecia (grade 2) Hyperkalemia (grade 2) Sores mouth (grade 2) Shortness of breath (grade 2) Dizziness (grade 2) Nausea (grade 2) Vomiting (grade 2) Ataxia (grade 2) Abdominal pain (grade 2) Headache (grade 2) Dehydration (grade 2) Sources: https://pubmed.ncbi.nlm.nih.gov/21625235
1400 mg 2 times / day steady, oral Dose: 1400 mg, 2 times / day Route: oral Route: steady Dose: 1400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/21625235	unhealthy, 61 years (range 33–79 years) Health Status: unhealthy Age Group: 61 years (range 33–79 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/21625235	DLT: Creatinine increased... Other AEs: Hypotension... Dose limiting toxicities: Creatinine increased (grade 2, 1 patient) Other AEs: Hypotension (grade 4, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/21625235
300 mg/m2 2 times / day steady, oral Recommended Dose: 300 mg/m2, 2 times / day Route: oral Route: steady Dose: 300 mg/m2, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20860038/	unhealthy, 8.5 years (range: 1.5-15 years) Health Status: unhealthy Age Group: 8.5 years (range: 1.5-15 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/20860038/	DLT: Skin rash, Mucositis... Other AEs: Nausea, Vomiting... Dose limiting toxicities: Skin rash (grade 3, 1 patient) Mucositis (grade 3, 1 patient) Aspartate aminotransferase increased (grade 3, 1 patient) Anorexia (grade 3, 1 patient) Hyperbilirubinemia (grade 3, 1 patient) Other AEs: Nausea (grade 1, 1 patient) Vomiting (grade 1, 1 patient) Fatigue (grade 1, 1 patient) Alanine aminotransferase increase (grade 1, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/20860038/

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252	inhibitor 2438	substrate 1388 inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C8 1057 P-gp 1741 MRP1 116 MRP3 246 MRP4 290	P-gp 2052

Drug as perpetrator

Target	Modality	Activity
P-gp 1932	inhibitor 4027 Sources: https://onlinelibrary.wiley.com/doi/10.1002/med.21510 Page: -	yes [IC50 3.7 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/18725460/ Page: -	yes
CYP2C9 2497	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/18725460/ Page: -	yes
CYP2D6 2546	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/18725460/ Page: -	yes
CYP3A4 2633	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/18725460/ Page: -	yes
MRP1 232	inhibitor 4027 Sources: https://onlinelibrary.wiley.com/doi/10.1002/med.21510 Page: -	yes
MRP3 326	inhibitor 4027 Sources: https://onlinelibrary.wiley.com/doi/10.1002/med.21510 Page: -	yes
MRP4 345	inhibitor 4027 Sources: https://onlinelibrary.wiley.com/doi/10.1002/med.21510 Page: -	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16544144/ Page: -	major
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/16544144/ Page: -	yes	no (pharmacogenomic study) Comment: CYP2D6 genetic polymorphism does not appreciably influence the pharmacokinetics of tipifarnib. Hence, concomitant administration of potent CYP2D6 inhibitors is anticipated to have little or no significant impact on the systemic exposure to tipifarnib. Sources: https://pubmed.ncbi.nlm.nih.gov/16544144/ Page: -
P-gp 2052	substrate 4014 Sources: https://link.springer.com/article/10.1023%2FB%3ADRUG.0000026254.97350.fe Page: -	yes	yes (pharmacogenomic study) Comment: Overall, this study indicates that ABCB1 genotype might be correlated with tipifarnib pharmacokinetics Sources: https://link.springer.com/article/10.1023%2FB%3ADRUG.0000026254.97350.fe Page: -

PubMed

Title	Date	PubMed
Farnesyltransferase inhibitor tipifarnib (R115777) preferentially inhibits in vitro autonomous erythropoiesis of polycythemia vera patient cells.	2005-05-01	15632209
Synthesis, biodistribution and effects of farnesyltransferase inhibitor therapy on tumour uptake in mice of 99mTc labelled epidermal growth factor.	2005-02	15657509
The American Society of Hematology--46th Annual Meeting and Exposition. HDAC, Flt and farnesyl transferase inhibitors.	2005-01	15650931
Farnesyltransferase inhibitor therapy in acute myelogenous leukemia.	2005-01	15610664
Dose-ranging pharmacodynamic study of tipifarnib (R115777) in patients with relapsed and refractory hematologic malignancies.	2004-12-01	15570084
The influence of farnesyl protein transferase inhibitor R115777 (Zarnestra) alone and in combination with purine nucleoside analogs on acute myeloid leukemia progenitors in vitro.	2004-12	15522064
Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors.	2004-11-01	15454229
Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.	2004-11-01	15454228
Gateways to clinical trials.	2004-11	15632957
[Multiple myeloma: from molecular pathogenensis to the development of molecular targeting therapies].	2004-11	15609681
Clinical activity of farnesyl transferase inhibitors in hematologic malignancies: possible mechanisms of action.	2004-11	15512806
Phase III double-blind placebo-controlled study of farnesyl transferase inhibitor R115777 in patients with refractory advanced colorectal cancer.	2004-10-01	15459217
The farnesyl transferase inhibitor R115777 (Zarnestra) synergistically enhances growth inhibition and apoptosis induced on epidermoid cancer cells by Zoledronic acid (Zometa) and Pamidronate.	2004-09-09	15286715
Gateways to clinical trials.	2004-09-07	15349141
Gateways to clinical trials.	2004-09	15538546
Investigation of the effect of the farnesyl protein transferase inhibitor R115777 on isoprenylation and intracellular signalling by the prostacyclin receptor.	2004-09	15339863
Quantile estimation following non-parametric phase I clinical trials with ordinal response.	2004-08-30	15287079
Microarray analysis reveals genetic pathways modulated by tipifarnib in acute myeloid leukemia.	2004-08-25	15329151
Phase II study of the farnesyl transferase inhibitor R115777 in patients with sensitive relapse small-cell lung cancer.	2004-08	15277257
Influence of farnesyl transferase inhibitor treatment on epidermal growth factor receptor status.	2004-08	15246358
Pharmacogenetics of tipifarnib (R115777) transport and metabolism in cancer patients.	2004-08	15122075
Farnesyltransferase inhibitors as anticancer agents: critical crossroads.	2004-07	15338957
Studies of the isoprenoid-mediated inhibition of mevalonate synthesis applied to cancer chemotherapy and chemoprevention.	2004-07	15229351
Farnesyl transferase inhibitors for patients with lung cancer.	2004-06-15	15217969
Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity.	2004-06-08	15170324
Gateways to clinical trials.	2004-06	15319815
Phase I and pharmacokinetic study of the farnesyltransferase inhibitor R115777 in combination with irinotecan in patients with advanced cancer.	2004-06	14760509
Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma.	2004-05-01	14726402
Farnesyl transferase inhibitor R115777 in myelodysplastic syndrome.	2004-05	15087061
Phase I and pharmacokinetic study of irinotecan in combination with R115777, a farnesyl protein transferase inhibitor.	2004-04-19	15083177
Phase III trial of gemcitabine plus tipifarnib compared with gemcitabine plus placebo in advanced pancreatic cancer.	2004-04-15	15084616
Phase II study of R115777, a farnesyl transferase inhibitor, in myelodysplastic syndrome.	2004-04-01	15051776
Targeted therapies in myelodysplastic syndromes: ASH 2003 review.	2004-04	15190511
Gateways to clinical trials.	2004-04	15148527
Gateways to clinical trials.	2004-03	15071612
R115777 induces Ras-independent apoptosis of myeloma cells via multiple intrinsic pathways.	2004-02	14985458
[Molecular pathogenesis of chronic myeloid leukemia and tyrosine kinase inhibitor].	2004-01	14999931
New targets for therapy in breast cancer: farnesyltransferase inhibitors.	2004	15535857
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.	2003-12-15	14643327
4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.	2003-12-15	14643326
Farnesyltransferase inhibitor R115777 in myelodysplastic syndrome: clinical and biologic activities in the phase 1 setting.	2003-12-15	12947010
The farnesyltransferase inhibitor R115777 reduces hypoxia and matrix metalloproteinase 2 expression in human glioma xenograft.	2003-12-01	14676133
Gateways to clinical trials.	2003-11	14685303
A phase I, pharmacokinetic, and biological study of the farnesyltransferase inhibitor tipifarnib in combination with gemcitabine in patients with advanced malignancies.	2003-10-15	14581347
Farnesyltransferase inhibitors and their potential in the treatment of breast carcinoma.	2003-10	14613029
Molecular neuro-oncology and development of targeted therapeutic strategies for brain tumors. Part 1: Growth factor and Ras signaling pathways.	2003-10	14599084
Primary and secondary prevention of non-small-cell lung cancer: the SPORE Trials of Lung Cancer Prevention.	2003-09	14641993
Gateways to clinical trials.	2003-09	14571286
Effects of the farnesyl transferase inhibitor R115777 on normal and leukemic hematopoiesis.	2003-09	12970780
Farnesyltransferase inhibitors in acute myeloid leukemia and myelodysplastic syndromes.	2003-08	14556673

Patents

Sample Use Guides

In Vivo Use Guide

Acute myeloid leukemia: 600 mg orally twice a day should be administered for the first 21 consecutive days, in 28-day cycles. Colorectal cancer: 300 mg should be given twice daily orally for 21 days every 28 days. Pancreatic cancer: tipifarnib is given at 200 mg twice daily orally continuously in combination with gemcitabine (1,000 mg/m(2) intravenously weekly x 7 for 8 weeks, then weekly x 3 every 4 weeks).

Route of Administration: Oral

In Vitro Use Guide

Tipifarnib was added to different cancer cell lines at concentrations ranging from 0.5–500 nm in 3 ul of DMSO. Cells were allowed to proliferate to high saturation densities beyond confluence for 4–7 days. The lowest IC50s were: 9.5 nM for SU86.86 (pancreatic cancer cell line with K-Ras mutation), 1.7 nM for HT-1197 (bladder cancer cell line with H-Ras mutation), 3.2 nM for WM-115 (melnoma, wild type), 6.5 nM for NCI-H292 (lung cancer cell line, wild type) and 3.9 nM for A673 (Rhabdomyo-sarcoma cell line, wild type).

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:08:48 GMT 2025` Edited by `admin` on `Mon Mar 31 18:08:48 GMT 2025`
Record UNII	MAT637500A
Record Status	`Validated (UNII)`
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Name

Type

Language

TIPIFARNIB

Official Name

English

ZARNESTRA

Preferred Name

English

2 (1H))-QUINOLINONE,6-(AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL)-4-(3-CHLOROPHENYL)-1-METHYL-,(+)-

Common Name

English

TIPIFARNIB [MI]

Common Name

English

(R)-6-[Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone

Systematic Name

English

NSC-702818

Code

English

TIPIFARNIB [MART.]

Common Name

English

tipifarnib [INN]

Common Name

English

R115777

Code

English

Tipifarnib [WHO-DD]

Common Name

English

R-115777

Code

English

R-11577

Code

English

TIPIFARNIB [USAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C2020