Delving into the Latest Updates on Toceranib with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

PHA-291639, SU 11654, SU-11654

Target

c-Kit

Action

inhibitors

Mechanism

c-Kit inhibitors(Stem cell growth factor receptor inhibitors)

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication-

Originator Organization

Sugen, Inc.

Active Organization

Sugen, Inc.

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC22H28FN4O6P

InChIKeyAOORBROPMMRREB-HBPAQXCTSA-N

CAS Registry874819-74-6

Medical records of dogs diagnosed with a high‐risk adrenocortical carcinoma (ACC) or phaeochromocytoma (PCC), treated with toceranib, were retrospectively reviewed. High‐risk ATs were defined as inoperable and/or metastatic ATs or cortical tumours with high Utrecht score. Endpoints were response rate, TTP and overall progression‐free survival time (PFST). Adverse events were reported according to VCOG‐CTCAE.

Results:

Sixteen dogs were included: 10 diagnosed with PCC and six with ACC. All dogs with ACC received adjuvant toceranib due to a high Utrecht score or metastatic disease, while all dogs with PCC were treated with toceranib in the macroscopic setting. A clinical benefit was detected in 80% of dogs with PCC: four achieved stable disease for a median TTP of 176.5 days, and two achieved partial response for 182 and >100 days, respectively. Median PFST for dogs with PCC was 112 days. Among dogs with ACC, 3 (50%) progressed and were euthanized after 237, 364 and 273 days; the remaining 3 (50%) dogs were alive and disease free 382, 508 and 583 days after starting toceranib. Overall, toceranib was well‐tolerated.

Clinical Significance:

Toceranib may offer clinical benefit and improve outcome in dogs with high‐risk ATs in both the macroscopic and microscopic disease setting.

05 May 2025·MOLECULAR PHARMACEUTICS

Pilot Study of Intratumoral Immunotherapy with Cowpea Mosaic Virus Nanoparticles: Safety in Refractory Canine Oral Tumors

Article

Author: Beiss, Veronique ; Perisé-Barrios, Ana Judith ; Steinmetz, Nicole F. ; del Castillo Magan, Noemí ; Arias-Pulido, Hugo ; vom Berg, Johannes ; Schaafsma, Evelien ; Vázquez, Fernando ; Fiering, Steven ; Delgado-Bonet, Pablo ; Emilia Zimmermann, Anna Barbara

Oral tumors (squamous cell carcinoma, malignant melanoma, and fibrosarcoma) represent 6-7% of all canine cancers. Given that these tumors have a high local recurrence rate and metastatic potential, conventional therapies have suboptimal response rates, leading to poor patient outcomes. Here, we report the use of intratumoral virus-like particles from cowpea mosaic virus (CPMV) in four canine patients with recurrent oral malignant tumors and lymph node metastasis. All tumors were nonresponders to chemotherapy and had a mild initial response to CPMV intratumoral immunotherapy without any serious immune-related adverse effects. None of the patients developed pulmonary metastasis during follow-up, although local progression was seen in all the patients. Furthermore, tumor-infiltrated immune T cells increased in number after the intratumoral immunotherapy with CPMV, suggesting activation of the tumor microenvironment. All the patients had a rapid decrease in the tumor-promoting chemokines IL-8 and CXCL1, which could indicate that a decrease in metastatic potential could have been generated by the CPMV immunotherapy. The increased number of infiltrated immune cells, the decrease in some pro-tumoral chemokines, and the absence of adverse effects suggest that CPMV could be a safe treatment and should be further explored as a novel therapy for canine oral tumors.

01 May 2025·JOURNAL OF VETERINARY INTERNAL MEDICINE

Effect of the Vascular Endothelial Growth Factor Inhibitor Toceranib on Cardiac Function and Endothelial Dysfunction Biomarkers in Dogs With Cancer

Article

Author: Jaffe, Iris Z. ; Lopez, Katherine E. ; Meola, Dawn M. ; Camarda, Nicholas D. ; London, Cheryl A. ; Yang, Vicky K. ; Upshaw, Jenica N.

ABSTRACT:

Background:

Hypertension is documented in dogs with cancer receiving toceranib, but no studies have evaluated left ventricular (LV) systolic function and biomarkers of endothelial function.

Objectives:

To characterize changes in echocardiographic variables and biomarkers of endothelial function in dogs treated with toceranib.

Animals:

Twenty‐six client‐owned dogs with no evidence of pre‐existing cardiac disease or systemic hypertension are receiving a single agent toceranib for cancer treatment.

Methods:

Dogs were enrolled in this prospective observational study with study visits at baseline, 1, 3, and 5 months after starting toceranib for echocardiographic exams, blood and urine collection, and blood pressure measurements, with an additional blood pressure obtained 2 weeks after starting toceranib. Serum markers of vascular endothelial function (VEGF, endothelin‐1, platelet derived growth factor [PDGF], prostacyclin, cyclic guanosine monophosphate [cGMP]) and urinary nitrate were evaluated with ELISA.

Results:

Dogs were enrolled between 2019 and 2023. Systolic blood pressure increased 2 weeks after initiating toceranib treatment (p = 0.009). Serum prostacyclin concentration was lower after 1 month of treatment (mean 98.8 pg/mL vs. 140.0 pg/mL at baseline, p = 0.03), and serum VEGF concentration was higher after 3 months of treatment (mean of 247.8 pg/mL vs. 135.4 pg/mL at baseline, p = 0.01). Global longitudinal strain (GLS) decreased at the five‐month time point (mean −14.5% vs. −15.7% at baseline, p = 0.048) with no significant change in LV fractional shortening by M‐mode or ejection fraction by Simpson's method of discs.

Conclusions:

Dogs treated with toceranib might have higher systemic blood pressure associated with changes in VEGF and prostacyclin and decreased systolic function.

100 Deals associated with Toceranib

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