Page last updated: 2024-11-12

toceranib phosphate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

toceranib phosphate: a tyrosine kinase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16034840
CHEMBL ID2103833
MeSH IDM0538270

Synonyms (35)

Synonym
toceranib phosphate (usan)
D08544
874819-74-6
pha-291639e
toceranib phosphate [usan]
24f9pf7j3r ,
toceranib phosphate
su-11654
unii-24f9pf7j3r
su 11654
su11654
CHEMBL2103833
toceranib (phosphate)
HY-10330A
CS-1231
S5272
toceranib phosphate [green book]
(z)-5-((5-fluoro-2-oxo-1,2-dihydro-3h-indol-3-ylidene)methyl)-2,4-dimethyl-n-(2-pyrrolidin-1-ylethyl)-1h-pyrrole-3-carboxamide phosphate
1h-pyrrole-3-carboxamide, 5-((z)-(5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl)-2,4-dimethyl-n-(2-(1-pyrrolidinyl)ethyl)-, phosphate (1:1)
5-[(z)-(5-fluoro-2-oxo-1,2-dihydro-3h-indol-3-ylidene)methyl]-2,4-dimethyl-n-[2-(pyrrolidin-1-yl)ethyl]-1h-pyrrole-3-carboxamide phosphate (1:1)
toceranib phosphate [mi]
AKOS027427177
toceranib phosphate(su 11654)
mfcd25372034
(z)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-n-(2-(pyrrolidin-1-yl)ethyl)-1h-pyrrole-3-carboxamide phosphate
su11654 phosphate
pha 291639 phosphate
CCG-269649
Q27253845
5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-n-(2-pyrrolidin-1-ylethyl)-1h-pyrrole-3-carboxamide;phosphoric acid
AS-57142
AKOS037645104
pha291639
BT162330
5-((z)-(5-fluoro-2-oxo-1,2-dihydro-3h-indol-3-ylidene)methyl)-2,4-dimethyl-n-(2-(pyrrolidin-1-yl)ethyl)-1h-pyrrole-3-carboxamide phosphate (1:1)

Research Excerpts

Overview

Toceranib phosphate is a multi-target receptor tyrosine kinase (RTK) inhibitor. It could prove to be a useful postoperative adjuvant treatment because of its modulation of the TME.

ExcerptReferenceRelevance
"Toceranib phosphate (TOC) is a multi-target receptor tyrosine kinase (RTK) inhibitor that exhibits activity against members of the split kinase family of RTKs."( Characterization of receptor tyrosine kinase activation and biological activity of toceranib phosphate in canine urothelial carcinoma cell lines.
Breitbach, JT; Fenger, JM; Geisler, JA; Husbands, BD; Korec, DI; Louke, DS, 2021
)
1.57
"Toceranib phosphate could prove to be a useful postoperative adjuvant treatment because of its modulation of the TME."( Assessment of postoperative adjuvant treatment using toceranib phosphate against adenocarcinoma in dogs.
Akiyoshi, H; Mie, K; Miura, N; Nishida, H; Tanaka, T; Yamazaki, H, 2020
)
2.25

Effects

Toceranib phosphate has been reported to provide clinical benefit (CB) in dogs with thyroid carcinoma. Its role in treatment-naïve thyroid tumours has not been well-described.

ExcerptReferenceRelevance
"Toceranib phosphate (Palladia) has a reported objective response rate of 25% in both canine apocrine gland anal sac adenocarcinoma (AGASACA) and thyroid carcinoma (TC), with stable disease occurring in an additional 50-60% of dogs. "( Evaluation of expression and function of vascular endothelial growth factor receptor 2, platelet derived growth factor receptors-alpha and -beta, KIT, and RET in canine apocrine gland anal sac adenocarcinoma and thyroid carcinoma.
Kisseberth, WC; London, CA; Russell, DS; Urie, BK, 2012
)
1.82
"Toceranib phosphate has been licensed for the treatment of dogs with mast cell tumours."( The role of toceranib phosphate in dogs with non-mast cell neoplasia: A systematic review.
Frezoulis, P; Harper, A, 2022
)
1.82
"Toceranib phosphate has been reported to provide clinical benefit (CB) in dogs with thyroid carcinoma, while its role in treatment-naïve thyroid tumours has not been well-described."( Toceranib phosphate in the treatment of canine thyroid carcinoma: 42 cases (2009-2018).
Bello, NM; Biller, B; Hocker, S; Sheppard-Olivares, S; Szivek, A; Wood, E; Wouda, RM, 2020
)
2.72
"Toceranib phosphate has been shown to be an efficacious therapy for canine mast cell tumors with increasing evidence that it may be beneficial in the medical management of neuroendocrine tumors."( Long-Term Survival and Glycemic Control with Toceranib Phosphate and Prednisone for a Metastatic Canine Insulinoma.
Boudreaux, B; Flesner, BK; Fletcher, JM; Smithee, T,
)
1.11

Treatment

Toceranib phosphate (TOC) and firocoxib reduced the tumor size, which was defined as partial response (PR) Treatment with toceranib phosphatide was initiated and well tolerated by the animal.

ExcerptReferenceRelevance
"Toceranib phosphate treatment might result in increased systolic blood pressures in dogs. "( Effects of Toceranib Phosphate on Systolic Blood Pressure and Proteinuria in Dogs.
Markovic, LE; Stein, TJ; Stepien, RL; Tjostheim, SS, 2016
)
2.27
"Treatment with toceranib phosphate (TOC) and firocoxib reduced the tumor size, which was defined as partial response (PR)."( Toceranib phosphate and firocoxib-mediated partial response in a dog with advanced intranasal sarcoma.
Ikeda, M; Kimura, J; Kishimoto, M; Kondo, H; Kushida, K; Ohmori, K; Okazawa, T; Osada, H, 2023
)
2.69
"Treatment with toceranib phosphate was started."( Long-term clinical control of feline pancreatic carcinoma with toceranib phosphate.
Boudreaux, BB; Dedeaux, AM; Langohr, IM, 2018
)
1.06
"Treatment with toceranib phosphate, a tyrosine-kinase inhibitor, was initiated and well tolerated by the animal."( TREATMENT OF RENAL CARCINOMA IN A BINTURONG (ARCTICTIS BINTURONG) WITH NEPHRECTOMY AND A TYROSINE KINASE INHIBITOR.
Fitzgerald, SD; Harrison, T; Needle, D; Patterson, J; Thompson, KA, 2016
)
0.77
"Treatment with toceranib phosphate resulted in complete response, despite the absence of exon-8 or exon-11 c-kit mutation."( Successful treatment of a metastatic, gastrointestinal stromal tumour in a dog with toceranib phosphate (Palladia).
Baines, L; Elliott, JW; Parry, A; Swinbourne, F, 2017
)
1.02

Toxicity

ExcerptReferenceRelevance
" As concurrent use may be warranted for a given individual and the adverse event (AE) profile for each can be overlapping (gastrointestinal), a phase I trial was performed in tumour-bearing (non-mast cell) dogs to establish the safety of the combination using a standard 3+3 cohort design."( Safety evaluation of combination toceranib phosphate (Palladia®) and piroxicam in tumour-bearing dogs (excluding mast cell tumours): a phase I dose-finding study.
Chon, E; Kubicek, LN; McCartan, L; Vail, DM, 2012
)
0.66
" Preliminary data suggests that lower doses of toeceranib may be associated with a reduced adverse event profile while maintaining sufficient drug exposure to provide biologic activity."( Evaluation of the adverse event profile and pharmacodynamics of toceranib phosphate administered to dogs with solid tumors at doses below the maximum tolerated dose.
Bernabe, LF; Kisseberth, WC; London, CA; Nguyen, S; Pennell, M; Portela, R; Yancey, MF, 2013
)
0.63
" Response to therapy was assessed using standard RECIST criteria and adverse events were characterized using the VCOG-CTCAE."( Evaluation of the adverse event profile and pharmacodynamics of toceranib phosphate administered to dogs with solid tumors at doses below the maximum tolerated dose.
Bernabe, LF; Kisseberth, WC; London, CA; Nguyen, S; Pennell, M; Portela, R; Yancey, MF, 2013
)
0.63
"9 mg/kg every other day provide drug exposure considered sufficient for target inhibition while resulting in an adverse event profile substantially reduced from that associated with the label dose of toceranib."( Evaluation of the adverse event profile and pharmacodynamics of toceranib phosphate administered to dogs with solid tumors at doses below the maximum tolerated dose.
Bernabe, LF; Kisseberth, WC; London, CA; Nguyen, S; Pennell, M; Portela, R; Yancey, MF, 2013
)
0.63
" Toxicity was graded according to the Veterinary Comparative Oncology Group - common terminology criteria for adverse events(VCOG-CTCAE) and response was measured according to Response Evaluation In Solid Tumors (RECIST) criteria."( Toxicity and response in cats with neoplasia treated with toceranib phosphate.
Blackwood, L; Harper, A, 2017
)
0.7
" Toxicities were graded using the Veterinary Cooperative Oncology Group - Common Terminology Criteria for Adverse Events criteria and compared to published data on TOC-associated GI toxicity."( Increased incidence of gastrointestinal toxicity in canine cancer patients treated with concurrent abdominal radiation therapy and toceranib phosphate.
Boss, MK; LaRue, SM; Leary, D; Martin, T; Prebble, AR; Thamm, DH; Weishaar, KM, 2022
)
0.93
" This study aimed to determine the tolerability and adverse event profile of combined toceranib and low dose meloxicam in cancer-bearing cats."( Low dose meloxicam is safe and tolerable when combined with toceranib phosphate in cancer-bearing cats.
Keepman, SJ; Pellin, MA, 2022
)
0.96
"02 mg/kg q24h was safe and well tolerated, with no cats being withdrawn due to adverse events from the drug combination."( Low dose meloxicam is safe and tolerable when combined with toceranib phosphate in cancer-bearing cats.
Keepman, SJ; Pellin, MA, 2022
)
0.96
"Low dose meloxicam combined with toceranib is safe and well tolerated in cancer-bearing cats."( Low dose meloxicam is safe and tolerable when combined with toceranib phosphate in cancer-bearing cats.
Keepman, SJ; Pellin, MA, 2022
)
0.96

Compound-Compound Interactions

ExcerptReferenceRelevance
" The immunomodulatory effects of the TKI toceranib, as a single agent or in combination with metronomic CYC, have not been previously investigated in dogs."( Clinical and immunomodulatory effects of toceranib combined with low-dose cyclophosphamide in dogs with cancer.
Biller, BJ; Mitchell, L; Thamm, DH,
)
0.13
"In addition to antitumor effects, these data support further investigations into the immunomodulatory effects of toceranib, administered alone or in combination with CYC in dogs with cancer."( Clinical and immunomodulatory effects of toceranib combined with low-dose cyclophosphamide in dogs with cancer.
Biller, BJ; Mitchell, L; Thamm, DH,
)
0.13
"To compare survival in dogs with recurrent or metastatic insulinomas that were treated with palliative therapy, alone or in combination with toceranib phosphate and to assess tolerability of the combined therapy in dogs."( Evaluation of palliative therapy, alone or in combination with toceranib phosphate, in dogs diagnosed with metastatic or recurrent beta-cell neoplasia.
Alonso-Miguel, D; Clarés Moral, I; García-San José, P; González Sanz, S; Pérez-Alenza, MD, 2021
)
1.06
"The use of toceranib combined with palliative treatment in dogs with suspect metastatic or recurrent insulinomas increased survival time and was adequate tolerated."( Evaluation of palliative therapy, alone or in combination with toceranib phosphate, in dogs diagnosed with metastatic or recurrent beta-cell neoplasia.
Alonso-Miguel, D; Clarés Moral, I; García-San José, P; González Sanz, S; Pérez-Alenza, MD, 2021
)
0.86
"Low dose meloxicam combined with toceranib is safe and well tolerated in cancer-bearing cats."( Low dose meloxicam is safe and tolerable when combined with toceranib phosphate in cancer-bearing cats.
Keepman, SJ; Pellin, MA, 2022
)
0.96

Bioavailability

ExcerptReferenceRelevance
" Oral bioavailability was 76."( Pharmacokinetic properties of toceranib phosphate (Palladia, SU11654), a novel tyrosine kinase inhibitor, in laboratory dogs and dogs with mast cell tumors.
Boucher, JF; Lesman, SP; Merritt, DA; Michels, GM; Yancey, MF, 2010
)
0.65

Dosage Studied

ExcerptRelevanceReference
" Five dose-escalating cohorts, up to and including approved label dosage for toceranib and standard dosage for piroxicam, were completed without observing a frequency of dose-limiting AEs necessitating cohort closure."( Safety evaluation of combination toceranib phosphate (Palladia®) and piroxicam in tumour-bearing dogs (excluding mast cell tumours): a phase I dose-finding study.
Chon, E; Kubicek, LN; McCartan, L; Vail, DM, 2012
)
0.66
"7%) were dosed on a Monday/Wednesday/Friday basis and 47/63 (74."( Preliminary evidence for biologic activity of toceranib phosphate (Palladia(®)) in solid tumours.
Alvarez, F; Beaver, L; Bryan, J; Carreras, J; Clifford, C; Ettinger, S; Fulton, L; Gauthier, M; Gill, V; Gillings, S; Haney, S; Henry, C; Hershey, B; Higginbotham, ML; Hillman, L; Jones, P; Kiselow, M; Klein, MK; Krick, E; Ladue, T; London, C; Mathie, T; McNeill, C; Novasad, A; Phillips, B; Stingle, N; Thamm, D; Vail, DM; Vaughan, A; Vickery, K, 2012
)
0.64
"Tyrosine kinase inhibitors (TKIs) and metronomic dosing of cyclophosphamide (CYC) can improve tumor control by suppression of regulatory T cells (Treg) and restoration of T cell-mediated immune responses in mice and humans."( Clinical and immunomodulatory effects of toceranib combined with low-dose cyclophosphamide in dogs with cancer.
Biller, BJ; Mitchell, L; Thamm, DH,
)
0.13
"While maintaining a standard toceranib dosage [2."( Safety evaluation of combination CCNU and continuous toceranib phosphate (Palladia(®) ) in tumour-bearing dogs: a phase I dose-finding study.
Kurzman, ID; Pan, X; Tsimbas, K; Vail, DM, 2016
)
0.68
" Low-dose aspirin was started in addition to an increased dosage of enalapril (0."( Toceranib phosphate-associated nephrotic syndrome in a dog: a case report.
Donnelly, LL; Herrera, CL; Remerowski, SM, 2021
)
2.06
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (94)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (6.38)29.6817
2010's58 (61.70)24.3611
2020's30 (31.91)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.04

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index53.04 (24.57)
Research Supply Index4.77 (2.92)
Research Growth Index5.41 (4.65)
Search Engine Demand Index119.24 (26.88)
Search Engine Supply Index2.87 (0.95)

This Compound (53.04)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials17 (17.00%)5.53%
Reviews3 (3.00%)6.00%
Case Studies17 (17.00%)4.05%
Observational0 (0.00%)0.25%
Other63 (63.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]