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Therapy Name | Vandetanib |
Synonyms | |
Therapy Description |
Caprelsa (vandetanib) is a multi-tyrosine kinase inhibitor with activity against VEGFR, EGFR, RET, SRC, and ABL1 kinases, potentially resulting in decreased tumor growth (PMID: 25031937, PMID: 25490448). Caprelsa (vandetanib) is FDA approved for use in medullary thyroid cancer (FDA.gov). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Vandetanib | Caprelsa | ZD6474|AZD6474|AZD 6474 | ABL1 Inhibitor 8 EGFR Inhibitor (Pan) 62 RET Inhibitor 53 SRC Inhibitor 31 VEGFR Inhibitor (Pan) 36 | Caprelsa (vandetanib) is a multi-tyrosine kinase inhibitor with activity against VEGFR, EGFR, RET, SRC, and ABL1 kinases, potentially resulting in decreased tumor growth (PMID: 25031937, PMID: 25490448). Caprelsa (vandetanib) is FDA approved for use in medullary thyroid cancer (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
RET M918T | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited Ret autophosphorylation and transforming activity in cells expressing RET M918T in culture (PMID: 15184865). | 15184865 |
RET L790F | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited Ret autophosphorylation in transformed cells expressing RET L790F in culture (PMID: 15184865). | 15184865 |
RET C634R | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited RET phosphorylation and decreased growth of transformed cells expressing RET C634R in culture (PMID: 15184865). | 15184865 |
RET C634R | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical - Cell culture | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited Ret phosphorylation and proliferation in a transformed cell line expressing RET C634R in culture (PMID: 37535881). | 37535881 |
RET M918T | lung small cell carcinoma | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited growth of small cell lung carcinoma lines expressing RET M918T (PMID: 25122427). | 25122427 |
RET wild-type | lung small cell carcinoma | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited growth of small cell lung carcinoma lines expressing wild-type RET (PMID: 25122427). | 25122427 |
RET D898_E901del | Advanced Solid Tumor | predicted - sensitive | Vandetanib | Preclinical - Cell culture | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited Ret phosphorylation and proliferation in a transformed cell line expressing RET D898_E901del, but to a lesser degree than cells expressing RET C634R in culture (PMID: 37535881). | 37535881 |
ALK F1174L | neuroblastoma | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) treatment resulted in decreased tumor weight in a Mycn-overexpressing neuroblastoma transgenic mouse model with ALK F1174L (corresponds to F1178L in mouse) and subsequent upregulation of Ret (PMID: 24811913). | 24811913 |
RET V804M | Advanced Solid Tumor | resistant | Vandetanib | Preclinical | Actionable | In a preclinical study, transformed cells expressing RET V804M demonstrated resistance to growth inhibition by Caprelsa (vandetanib) in culture (PMID: 15184865). | 15184865 |
RET Y791F | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited Ret autophosphorylation in transformed cells expressing RET Y791F in culture (PMID: 15184865). | 15184865 |
ALK R1275Q | neuroblastoma | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) treatment resulted in decreased tumor weight in a Mycn-overexpressing neuroblastoma transgenic mouse model with ALK R1275Q (corresponds to R1279Q in mouse) and subsequent upregulation of Ret (PMID: 24811913). | 24811913 |
RET C634R RET Y806C | Advanced Solid Tumor | resistant | Vandetanib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells co-expressing RET C634R and RET Y806C were resistant to treatment with Caprelsa (vandetanib) in culture (PMID: 19029224). | 19029224 |
RET fusion | lung non-small cell carcinoma | sensitive | Vandetanib | Phase II | Actionable | In a Phase II trial, Caprelsa (vandetanib) treatment resulted in a disease control rate of 88% (15/17), median progression-free survival (PFS) of 4.7 months, and partial response in 53% (9/17) of non-small cell lung adenocarcinoma patients harboring RET fusions (J Clin Oncol 34, 2016 (suppl; abstr 9012)). | detail... |
RET fusion | lung non-small cell carcinoma | sensitive | Vandetanib | Phase II | Actionable | In a Phase II trial, Caprelsa (vandetanib) treatment resulted in partial remission in 17% (3/18) and stable disease in 44% (8/18) of non-small cell lung adenocarcinoma patients harboring RET fusions (J Clin Oncol 34, 2016 (suppl; abstr 9013)). | detail... |
RET S891A | medullary thyroid carcinoma | predicted - sensitive | Vandetanib | Case Reports/Case Series | Actionable | In a clinical case study, neoadjuvant Caprelsa (vandetanib) treatment resulted in a 65% decrease in the thyroid mass and cervical lymph nodes allowing for surgical resection in a pediatric patient with medullary thyroid carcinoma harboring RET S891A (PMID: 38207224). | 38207224 |
RET D378_G385delinsE | medullary thyroid carcinoma | predicted - sensitive | Vandetanib | Case Reports/Case Series | Actionable | In a clinical case study, Caprelsa (vandetanib) treatment resulted in an ongoing biochemical response for more than 6 months in a pediatric patient 16 years old with metastatic medullary thyroid carcinoma harboring RET D378_G385delinsE (PMID: 28209747). | 28209747 |
RET A883F | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited Ret autophosphorylation in transformed cells expressing RET A883F in culture (PMID: 15184865). | 15184865 |
RET D898_E901del | medullary thyroid carcinoma | predicted - resistant | Vandetanib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with metastatic medullary thyroid carcinoma harboring RET D898_E901del demonstrated primary resistance to Caprelsa (vandetanib) treatment (PMID: 37535881). | 37535881 |
RET C634R RET Y806F | Advanced Solid Tumor | predicted - sensitive | Vandetanib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells co-expressing RET C634R and RET Y806F in culture demonstrated inhibition of Ret phosphorylation and activity in kinase assays when treated with Caprelsa (vandetanib) (PMID: 19029224). | 19029224 |
RET L633_A639del | medullary thyroid carcinoma | predicted - sensitive | Vandetanib | Case Reports/Case Series | Actionable | In a clinical case study, Caprelsa (vandetanib) treatment resulted in disease stabilization in a patient with metastatic medullary thyroid carcinoma harboring RET L633_A639del (PMID: 28209747). | 28209747 |
RET rearrange | lung non-small cell carcinoma | sensitive | Vandetanib | Phase II | Actionable | In a Phase II trial, treatment with Caprelsa (vandetanib) resulted in an objective response rate of 18% (3/17, all partial responses) and disease control rate of 65% (stable disease in 47% (8/17) + partial response in 18% (3/17)) and median progression-free survival of 4.5 months in patients with RET-rearranged metastatic or recurrent non-small cell lung cancer (PMID: 27803005; NCT01823068). | 27803005 |
RET rearrange | lung non-small cell carcinoma | sensitive | Vandetanib | Clinical Study | Actionable | In a clinical study, analysis of patients with RET-rearranged non-small cell lung cancer treated with RET inhibitors demonstrated a response rate of 18% (2/11, all partial responses) and stable disease in 27% (3/11) of patients following Caprelsa (vandetanib) treatment (PMID: 28447912). | 28447912 |
RET C634R RET V804M | Advanced Solid Tumor | resistant | Vandetanib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells co-expressing RET C634R and RET V804M were resistant to treatment with Caprelsa (vandetanib) in culture (PMID: 19029224). | 19029224 |
APC inact mut | colon cancer | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) reduced the number of dextran sodium sulfate-induced tumors in an APC-deficient mouse model for colon cancer (PMID: 20811697). | 20811697 |
RET C634R RET V804G | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, transformed cell lines expressing Ret protein carrying both C634R and V804G mutations were more sensitive to Vandetanib induced inhibition of Ret activity than cells expressing Ret C634R alone in culture (PMID: 15184865). | 15184865 |
RET E768D | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited Ret autophosphorylation in transformed cells expressing RET E768D in culture (PMID: 15184865). | 15184865 |
RET C634R RET Y806E | Advanced Solid Tumor | resistant | Vandetanib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells co-expressing RET C634R and RET Y806E were resistant to treatment with Caprelsa (vandetanib) in culture (PMID: 19029224). | 19029224 |
RET S891A | Advanced Solid Tumor | sensitive | Vandetanib | Preclinical | Actionable | In a preclinical study, Caprelsa (vandetanib) inhibited Ret autophosphorylation in transformed cells expressing RET S891A in culture (PMID: 15184865). | 15184865 |
RET V804L | Advanced Solid Tumor | resistant | Vandetanib | Preclinical | Actionable | In a preclinical study, transformed cells expressing RET V804L demonstrated resistance to growth inhibition by Caprelsa (vandetanib) in culture (PMID: 15184865). | 15184865 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01876784 | Phase III | Vandetanib | Evaluation of Efficacy, Safety of Vandetanib in Patients With Differentiated Thyroid Cancer | Completed | USA | SWE | POL | ITA | FRA | ESP | DNK | CZE | BRA | 3 |
NCT01934335 | Phase I | Vandetanib | Effect of Vandetanib on Cellular Markers in Invasive Breast Cancer | Terminated | USA | 0 |
NCT01585415 | Phase I | Vandetanib | Vemurafenib and White Blood Cell Therapy for Advanced Melanoma | Terminated | USA | 0 |
NCT01414426 | Phase II | Vandetanib | Vandetanib in Preventing Head and Neck Cancer in Patients With Precancerous Head and Neck Lesions | Completed | USA | 0 |
NCT02788201 | Phase II | Erlotinib Thiotepa Imatinib Dacarbazine Arsenic trioxide Idarubicin Mitomycin C Thioguanine Mercaptopurine Methotrexate Cladribine Epirubicin Gemcitabine Doxorubicin Bleomycin Etoposide Gefitinib Daunorubicin Lomustine Sorafenib Sunitinib Ifosfamide Asparaginase Ixabepilone Abiraterone Azacitidine Ruxolitinib Decitabine Axitinib Estramustine Floxuridine Lapatinib Carmustine Fludarabine Nilotinib Cisplatin Vismodegib Vandetanib Melphalan Busulfan Carboplatin Toremifene Crizotinib Dactinomycin Temsirolimus Vorinostat Romidepsin Fluorouracil Irinotecan Bortezomib Tamoxifen Topotecan Chlorambucil Pentostatin Eribulin Carfilzomib Vemurafenib Hydroxyurea Exemestane Vincristine Sulfate Dasatinib Mitoxantrone Vinblastine Cytarabine Tretinoin Clofarabine Teniposide Docetaxel Pazopanib Oxaliplatin Streptozocin Paclitaxel Bendamustine Mechlorethamine Mitotane | Genomic Based Assignment of Therapy in Advanced Urothelial Carcinoma | Completed | USA | 0 |
NCT04760288 | Phase III | Cabozantinib Pralsetinib Vandetanib | A Study of Pralsetinib Versus Standard of Care (SOC) for Treatment of RET-Mutated Medullary Thyroid Cancer (MTC). (AcceleRET-MTC) | Withdrawn | ESP | 0 |
NCT00566995 | Phase II | Vandetanib | Phase II Study of Vandetanib in Individuals With Kidney Cancer | Completed | USA | 0 |
NCT02015065 | Phase II | Vandetanib | Phase II Trial of Vandetanib in Children and Adults With Wild-Type Gastrointestinal Stromal Tumors | Completed | USA | 0 |
NCT04211337 | Phase III | Vandetanib Cabozantinib Selpercatinib | A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer (LIBRETTO-531) | Active, not recruiting | USA | POL | NLD | ITA | ISR | GRC | GBR | FRA | ESP | DEU | CZE | CAN | BRA | BEL | AUS | 5 |