Therapy Detail

Therapy Name Dovitinib
Therapy Description

Dovitinib (TKI258) targets multiple receptor tyrosine kinases including Flt3, c-Kit, CSF1R, FGFR 1-4, VEGFR 1-3, and PDGFR alpha and beta, potentially resulting in decreased tumor growth (PMID: 15598814, PMID: 25219510, PMID: 23658459, PMID: 16033847).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Dovitinib TKI258|CHIR-258 CSF1R Inhibitor 22 FGFR Inhibitor (Pan) 17 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 VEGFR Inhibitor (Pan) 29 Dovitinib (TKI258) targets multiple receptor tyrosine kinases including Flt3, c-Kit, CSF1R, FGFR 1-4, VEGFR 1-3, and PDGFR alpha and beta, potentially resulting in decreased tumor growth (PMID: 15598814, PMID: 25219510, PMID: 23658459, PMID: 16033847).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 N549K endometrial cancer decreased response Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) did not potently inhibit proliferation of endometrial cancer cell lines harboring FGFR2 N549K in cell culture (PMID: 22238366). 22238366
FGFR2 L618M Advanced Solid Tumor decreased response Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 L618M demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR3 N540K Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 N540K in culture (PMID: 28034880). 28034880
FGFR2 N550S Advanced Solid Tumor decreased response Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550S demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 amp breast cancer sensitive Dovitinib Preclinical - Pdx & cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell growth of an FGFR2 amplified breast cancer cell line in culture and prevented tumor growth and induced tumor regression in FGFR2 amplified breast cancer patient derived xenograft (PDX) models (PMID: 23658459). 23658459
FGFR2 V565I Advanced Solid Tumor resistant Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 V565I were resistant to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 I548V Advanced Solid Tumor decreased response Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 I548V demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR3 L608V Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 L608V in culture (PMID: 28034880). 28034880
FGFR3 over exp urinary bladder cancer sensitive Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 8% (1/13) of non-muscle invasive bladder cancer patients over expressing FGFR3 (J Clin Oncol 34, 2016 (suppl; abstr 4526)). detail...
FGFR2 S252W endometrial cancer decreased response Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) did not potently inhibit cell proliferation in endometrial cancer cells harboring FGFR2 S252W mutation in culture (PMID: 22238366). 22238366
FGFR3 K650E Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 K650E in culture (PMID: 28034880). 28034880
FGFR2 N550H Advanced Solid Tumor decreased response Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550H demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 M538I Advanced Solid Tumor decreased response Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M538I demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR1 amp estrogen-receptor positive breast cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in estrogen receptor (ER)-positive breast cancer cells harboring FGFR1 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp stomach cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in gastric cancer cell lines harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR2 amp myxoid liposarcoma sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) increased apoptosis, inhibited cell proliferation and migration of myxoid liposarcoma cell lines harbors FGFR2 amplification in culture (PMID: 26036639). 26036639
Unknown unknown melanoma not applicable Dovitinib Phase Ib/II Actionable In a Phase I/II study, Dovitinib (TKI258) was demonstrated safe, but of limited clinical benefit in patients with advanced melanoma (PMID: 21976540). 21976540
FGFR3-BAIAP2L1 urinary bladder cancer sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 S249C urinary bladder cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in bladder cancer cells harboring FGFR3 S249C mutation in culture (PMID: 22238366). 22238366
FGFR3 act mut Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR3 in culture (PMID: 22238366). 22238366
Unknown unknown gastrointestinal stromal tumor not applicable Dovitinib Phase II Actionable In a Phase II clinical trial, Dovitinib (TKI258) demonstrated safety and efficacy in heavily pretreated patients with advanced GISTs (PMID: 24084771). 24084771
FGFR3 S249C Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). 23786770
FGFR2 M536I Advanced Solid Tumor decreased response Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 M536I demonstrated a decreased response to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR3 V555M Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited proliferation of transformed cells over expressing FGFR3 V555M in culture (PMID: 28034880). 28034880
FGFR3 S249C bladder urothelial carcinoma sensitive Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response in a patient with BCG-unresponsive, non-muscle-invasive, urothelial carcinoma of the bladder harboring FGFR3 S249C (PMID: 27932416). 27932416
Unknown unknown glioblastoma multiforme not applicable Dovitinib Phase I Actionable In a Phase I trial, Dovitinib (TKI258) treatment resulted in a progression free survival rate at 6 months of 16.7% (2/12) in patients with recurrent glioblastoma (PMID: 27100354). 27100354
Unknown unknown renal cell carcinoma not applicable Dovitinib Phase I Actionable In a Phase I trial, Dovitinib (TKI258) demonstrated safety and efficacy resulting in 10% (2/20) partial response and 60% (12/20) stable disease in renal cell carcinoma patients (PMID: 23339124). 23339124
Unknown unknown renal cell carcinoma not applicable Dovitinib Phase III Actionable In a Phase III clinical trial, Dovitinib (TKI258) demonstrated efficacy equivalent to Nexavar (sorafenib) in metastatic renal cell carcinoma patients (PMID: 24556040). 24556040
FGFR2 E566G Advanced Solid Tumor resistant Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 E566G were resistant to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR1 amp lung squamous cell carcinoma no benefit Dovitinib Phase II Actionable In a Phase II clinical trial, dovitinib treatment resulted in a objective response rate of 11.5% (3/26, all partial responses) and disease control rate of 50% (13/26), and a median progression-free survival of 2.9 months in lung squamous cell carcinoma patients with FGFR1 amplification, and FGFR1 amplification was not determined to be a predictive biomarker for sensitivity (PMID: 27315356). 27315356
FGFR2 S252W Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 S252W were sensitive to Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR2 act mut endometrial cancer sensitive Dovitinib Preclinical - Cell line xenograft Actionable In a preclinical study, both cell lines and cell line xenograft models of endometrial cancer with FGFR2 activating mutations showed greater sensitivity to Dovitinib (TKI258) as compared to FGFR2 wild-type (PMID: 23443805). 23443805
FGFR3 R248C Advanced Solid Tumor sensitive Dovitinib Preclinical - Cell culture Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). 23786770
FGFR2 amp Her2-receptor positive breast cancer sensitive Dovitinib Phase I Actionable In a Phase I trial, Dovitinib (TKI258) displayed safety and preliminary efficacy resulting in tumor regression of 28.2% and 18.5% in two patients with FGFR2 amplified Erbb2 (Her2)-receptor positive breast cancer (PMID: 23658459). 23658459
FGFR2 N550K Advanced Solid Tumor resistant Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 N550K were resistant to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
FGFR3 Y375C urinary bladder cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in bladder cancer cells harboring FGFR3 Y375C in culture (PMID: 22238366). 22238366
RET G691S Advanced Solid Tumor sensitive Dovitinib Phase I Actionable In a Phase I clinical trial, two patients with germline RET G691S mutations demonstrated sensitivity to Dovitinib (TKI258) treatment (PMID: 25103625). 25103625
FGFR1 fusion Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited Erk, Stat5 signaling and survival of transformed cell lines overexpressing FGFR1 fusion proteins (ZMYM2-FGFR1 or BCR-FGFR1) in culture (PMID: 17698633). 17698633
FGFR3 mutant bladder urothelial carcinoma sensitive Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response in 33% (1/3) of patients with BCG-unresponsive, non-muscle-invasive, urothelial carcinoma of the bladder harboring FGFR3 mutations (PMID: 27932416). 27932416
FGFR2 amp colon cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited cell proliferation in colon cancer cells harboring FGFR2 amplification in culture (PMID: 22238366). 22238366
FGFR1 act mut Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). 22238366
FGFR1 fusion acute myeloid leukemia sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) increased apoptosis and inhibited survival of acute myelogenous leukemia cell lines harboring FGFR1OP2-FGFR1 fusion in culture (PMID: 17698633). 17698633
FGFR1 rearrange myeloproliferative neoplasm sensitive Dovitinib Preclinical Actionable In a preclinical study, primary cells from 8p11 myeloproliferative syndrome patients harboring FGFR1 rearrangement were sensitive to Dovitinib (TKI258)-induced growth inhibition in culture (PMID: 17698633). 17698633
FGFR1 amp Her2-receptor positive breast cancer sensitive Dovitinib Phase I Actionable In a Phase I trial, Dovitinib (TKI258) promoted 6-month stable disease in Erbb2 (Her2)-positive breast cancer patients with FGFR1 amplification (PMID: 23658459). 23658459
FGFR2 act mut Advanced Solid Tumor sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR2 in culture (PMID: 22238366). 22238366
FGFR3 mut FGFR3 over exp urinary bladder cancer sensitive Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment resulted in complete response for 6 months in 33% (1/3) of non-muscle invasive bladder cancer patients harboring both FGFR3 mutations and FGFR3 over expression (J Clin Oncol 34, 2016 (suppl; abstr 4526)). detail...
Unknown unknown adenoid cystic carcinoma not applicable Dovitinib Phase II Actionable In a Phase II trial, Dovitinib (TKI258) treatment was tolerated and demonstrated limited clinical activity in patients with adenoid cystic carcinoma, resulting in partial response in 5.9% (2/34) of patients, suppression of overall tumor growth rate, and a median progression-free survival of 8.2 months (PMID: 28377480). 28377480
FGFR3-TACC3 urinary bladder cancer sensitive Dovitinib Preclinical Actionable In a preclinical study, Dovitinib (TKI258) inhibited growth of bladder cancer cell lines that have been demonstrated to harbor FGFR3-TACC3 in culture (PMID: 24325461, PMID: 23175443). 23175443 24325461
FGFR2 K660E Advanced Solid Tumor resistant Dovitinib Preclinical Actionable In a preclinical study, transformed cells expressing FGFR2 K660E were resistant to treatment with Dovitinib (TKI258) (PMID: 23908597). 23908597
Clinical Trial Phase Therapies Title Recruitment Status
NCT01678105 Dovitinib A Phase II Study of Dovitinib in Recurrent and/or Metastatic Adenoid Cystic Carcinoma of the Salivary Glands Completed
NCT01994590 Phase II Dovitinib Dovitinib (TKI258) and Abiraterone Acetate in Metastatic Castrate-Resistant Prostate Cancer (mCRPC) Terminated
NCT01676714 Phase II Dovitinib Study of Dovitinib and Biomarkers in Advanced Non-Small Cell Lung Cancer or Advanced Colorectal Cancer Completed
NCT02048943 Phase I Dovitinib + Gemcitabine + Abraxane nab-paclitaxel Dovitinib Dovitinib Lactate, Gemcitabine Hydrochloride, and Paclitaxel Albumin-Stabilized Nanoparticle Formulation in Treating Patients With Advanced Solid Tumors or Pancreatic Cancer Withdrawn
NCT01497392 Phase I Gemcitabine Dovitinib Capecitabine Dovitinib Lactate, Gemcitabine Hydrochloride, and Capecitabine in Treating Patients With Advanced or Metastatic Solid Tumors, Pancreatic Cancer and Biliary Cancers Completed
NCT02108782 Phase II Dovitinib Dovitinib Lactate in Treating Patients With Pancreatic Neuroendocrine Tumors Withdrawn
NCT01266070 Dovitinib TKI 258 in Von Hippel-Lindau Syndrome (VHL) Terminated
NCT01262027 Phase II Dovitinib TKI258 for Metastatic Inflammatory Breast Cancer Patients Active, not recruiting
NCT01831726 Phase II Dovitinib Dovitinib for Patients With Tumor Pathway Activations Inhibited by Dovitinib Completed
NCT01769547 Phase II Dovitinib A Phase II Study of Single-agent DOVitinib in Advanced Malignant PlEural Mesothelioma Which Has Progressed Following Prior Platinum-Antifolate Chemotherapy Terminated
NCT01753713 Phase II Dovitinib Dovitinib in Treating Patients With Recurrent or Progressive Glioblastoma Completed
NCT01443481 Phase I Dovitinib Pharmacokinetics (PK) of TKI258 in Cancer Patients With Normal and Impaired Hepatic Function Completed
NCT02116803 Phase III Dovitinib An Open Label Multi-center Extension Study to Evaluate Long-term Safety/ Tolerability of Dovitinib in Patients With Solid Tumors Who Continue to Receive Treatment With Dovitinib (TKI258) in Novartis-sponsored Single Agent Dovitinib Studies Which Fulfilled the Requirements for the Primary Objective Completed
NCT01888965 Phase II Dovitinib Maintenance Dovitinib for Colorectal and Pancreas Cancer Terminated
NCT01484041 Phase Ib/II Dovitinib Dovitinib Plus an Aromatase Inhibitor for Metastatic Breast Cancer Terminated