Journal of Oncology / 2012 / Article / Tab 2

Review Article

Targeting the Tumor Microenvironment: Focus on Angiogenesis

Table 2

Summary of drugs, their revealed targets and indications in clinical trails. Drugs without a single treatment trial are marked with a “*”.

Drug (brand name, company)TargetApprovedClinical trials with single treatmentIndication

Bevacizumab (Avastin, Genentech/Roche)Monoclonal antibody against VEGFAmCRC, mRCC, NSCLC, metastatic HER2-negative breast cancer, glioblastomaPhase I, IIMultiple solid tumors (e.g., RCC, BC, pancreatic, prostate, ovarian, brain cancers) and hematologic malignancies (e.g., MM)

Sunitinib, SU11248 (Sutent, Pfizer)TKI of VEGFR 1–3, PDGFRα/β, c-Kit, Flt3, RET, CSF-1RmRCC, GISTPhase IMultiple solid tumors (e.g., RCC, BC, melanoma, lung)

Pazopanib (Votrient, GlaxoSmithKline)TKI of VEGFR 1–3, PDGFRα/β, c-kit tyrosine kinasesmRCCPhase I, IIMultiple solid tumors (e.g., BC, RCC, ovarian, lung) and others (e.g., lymphoma)

Sorafenib, BAY43-9006 (Nexavar, Bayer)TKI of Multiple cell surface kinases (VEGFR 1–3, RET, PDGFRβ, Flt-3, c-Kit, CSF-1) and intracellular kinases (CRAF, BRAF, mutant BRAF)mRCC, unresectable hepatocellular carcinomaPhase I, IIMultiple solid tumors (e.g., RCC, BC, melanoma, lung cancers) and hematologic malignancies (e.g., MM)

Vandetanib, ZD6474 (Zactima, AstraZeneca)TKI of VEGFR, EGFR and RETMetastatic medullary thyroid cancerPhase I, IINSCLC, RCC, glioblastoma

Bortezomib, PS-341 (Velcade, Millennium Pharmaceuticals)26S proteasome inhibitorMM, relapsed mantle cell lymphomaPhase I, IIMM, lymphoma, leukemia and multiple solid tumors (e.g., RCC, BC, lung, prostate)

Temsirolimus (Torisel, Wyeth)mTOR inhibitormRCCPhase I, IIMultiple solid tumors (e.g., RCC, BC, melanoma, prostate, liver cancers) and hematologic malignancies (e.g., lymphoma)

Everolimus, RAD001 (Afinitor, Novartis)mTOR inhibitorAdvanced renal cell carcinomaPhase I, IIMultiple solid tumors (e.g., BC, pancreatic, gastric cancers) and lymphoma

Thalidomide (Thalomid, Celgene)Angiogenesis inhibitor, multipleMM * MM

Lenalidomide, CC-5013 (Revlimid, Celgene)Angiogenesis inhibitor, Thalidomide derivativeMMPhase I, IIMM, lymphoma, chronic lymphocytic leukemia, and multiple solid tumors (e.g., CRC, ovarian)

Pomalidomide, CC-4047 (Actimid, Celgene)Angiogenesis inhibitor, Thalidomide derivativeNo yet approvedPhase IMM, Lymphoma

Aflibercept, VEGF-trap (ZALTRAP, Sanofi-Aventis and Regeneron)Decoy receptor for all VEGF-A isoformsNo yet approved * mCRC, RCC, Ovarian, NSCLC, prostate cancers, lymphoma, leukemia

Axitinib, AG-013736 (Pfizer)TKI of VEGFR 1–3, PDGFRβ, c-KIT and CSF-1No yet approvedPhase ImRCC, BC, NSCLC, metastatic pancreatic cancer, GIST, lung cancer, thyroid cancer

Icrucumab, IMC-18F1 (ImClone)Monoclonal antibody against VEGFR-1No yet approvedPhase IAdvanced solid tumors, (e.g., CRC, BC, carcinoma of urinary tract)

Ramucirumab, IMC-1121b (ImClone)Monoclonal antibody against VEGFR-2No yet approved * CRC, BC, mRCC, Advanced liver, gastric, prostate, ovarian, and NSCL cancers, melanoma

Vatalanib, PTK787 (Novartis)TKI of VEGFR 1–3, PDGFRα/β, and c-KITNot yet approved * Multiple solid tumors (e.g., CRC, glioblastoma, NSCLCs) and hematologic malignancies (e.g., leukemia)

Enzastaurin, LY317615.HCl (Eli Lilly)PKC inhibitorNot yet approved * BC, mCRC, Brain tumor, advanced NSCL, glioblastoma, lymphoma

Cediranib, AZD2171 (Recentin, AstraZeneca)TKI of VEGFR 1–3Not yet approvedPhase IRCC, CRC, BC, ovarian, prostate cancer, lung, brain, head and neck cancers, glioblastoma, melanoma

Vectibix, panitumumab (Amgen)EGFRmCRCPhase I, IImCRC, pancreatic, HNSCC, NSCLC, lung

Erbitux, cetuximab, (Imclone, Bristol-Myers Squibb)EGFRmCRCPhase I, IImCRC, HSNCC, brain, MM, lung, pancreatic, liver

Trastuzumab, herceptin (Genentech)HER2 receptorGastric cancer, HER2 positive BCPhase I, IIBC, gastric

Tykerb, lapatinib (GlaxoSmithKline)EGFR and HER2 receptorBCPhase I, IIBC, CRC, lung, HNSCC, pancreatic, melanoma

Tamoxifen, Novadex, Istubal, Valodex (AstraZeneca)Estrogen receptorBCPhase I, IIBC, bladder, melanoma, prostate

TKI: tyrosine kinase inhibitors; mCRC: metastatic colorectal cancer; NSCLC: nonsmall cell lung cancer; mRCC: metastatic renal cell carcinoma; GIST: gastrointestinal stroma tumor after progression; MM: multiple myeloma; BC: breast cancer; HNSCC: head and neck sequmous cell carcinoma.

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