Brivanib alaninate for cancer

Expert Opinion on Investigational Drugs

Volumn 20, Issue 4, 2011, Pages 577-586

  Diaz Padilla, Ivan ^a   Siu, Lillian L ^a  

^a PRINCESS MARGARET HOSPITAL   (Canada)

Author keywords

angiogenesis; brivanib; colorectal cancer; dynamic contrast enhanced magnetic resonance (DCE MRI); hepatocellular carcinoma

Indexed keywords

BRIVANIB; CETUXIMAB; FLUOROURACIL; FOLINIC ACID; IRINOTECAN; OXALIPLATIN; VASCULOTROPIN RECEPTOR;

AMINOTRANSFERASE BLOOD LEVEL; ANTINEOPLASTIC ACTIVITY; ARTERY THROMBOSIS; CANCER CHEMOTHERAPY; CANCER COMBINATION CHEMOTHERAPY; CANCER INHIBITION; CHEMOTHERAPY INDUCED EMESIS; COLORECTAL CANCER; COMPETITIVE INHIBITION; DEHYDRATION; DIARRHEA; DIGESTIVE SYSTEM CANCER; DRUG DOSE COMPARISON; DRUG DOSE ESCALATION; DRUG EFFICACY; DRUG INDUCED HEADACHE; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG STRUCTURE; DRUG TARGETING; DRUG TOLERABILITY; DRUG WITHDRAWAL; FATIGUE; HEMOGLOBIN BLOOD LEVEL; HUMAN; HYPERTENSION; HYPONATREMIA; IN VITRO STUDY; IN VIVO STUDY; LIVER CELL CARCINOMA; LOW DRUG DOSE; LUNG EMBOLISM; MENTAL DISEASE; MONOTHERAPY; NAUSEA; NONHUMAN; PHARMACODYNAMICS; REVIEW; SIDE EFFECT; TARGET ORGAN; THYROTROPIN BLOOD LEVEL; VENOUS THROMBOEMBOLISM;

ALANINE; ANGIOGENESIS INHIBITORS; ANIMALS; ANTINEOPLASTIC AGENTS; CLINICAL TRIALS AS TOPIC; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; NEOPLASMS; PYRROLES; RECEPTOR, FIBROBLAST GROWTH FACTOR, TYPE 1; TRIAZINES; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2;

EID: 79952690187     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.2011.565329     Document Type: Review

References (55)

1. Bergers G, Benjamin LE. Tumorigenesis and the angiogenic switch. Nat Rev Cancer 2003;20:401-10 (Pubitemid 37328844)
2. Ferrara N. VEGF and the quest for tumour angiogenesis factors. Nat Rev Cancer 2002;2:795-803 (Pubitemid 37328914)
3. Cook KM, Figg WD. Angiogenesis inhibitors: current strategies and future prospects. CA Cancer J Clin 2010;60:222-43
4. Posey JA, Ng TC, Yang B, et al. A Phase I study of anti-kinase insert domain-containing receptor antibody, IMC-1C11, in patients with liver metastases from colorectal carcinoma. Clin Cancer Res 2003;9:1323-32 (Pubitemid 36418382)
5. Spratlin JL, Cohen RB, Eadens M, et al. Phase I pharmacologic and biologic study of ramucirumab (IMC-1121B), a fully human immunoglobulin G1 monoclonal antibody targeting the vascular endothelial growth factor receptor-2. J Clin Oncol 2010;28:780-7
6. Tang JR, Markham NE, Lin YJ, et al. Inhaled nitric oxide attenuates pulmonary hypertension and improves lung growth in infant rats after neonatal treatment with a VEGF receptor inhibitor. Am J Physiol Lung Cell Mol Physiol 2004;287:L344-51
7. Izzedine H, Rixe O, Billemont B, et al. Angiogenesis inhibitor therapies: focus on kidney toxicity and hypertension. Am J Kidney Dis 2007;50:203-18 (Pubitemid 47095077)
8. Kerbel RS. Therapeutic implications of intrinsic or induced angiogenic growth factor redundancy in tumors revealed. Cancer Cell 2005;8:269-71 (Pubitemid 41443411)
9. Presta M, Dell'Era P, Mitola S, et al. Fibroblast growth factor/fibroblast growth factor receptor system in angiogenesis. Cytokine Growth Factor Rev 2005;16:159-78 (Pubitemid 40616114)
10. Turner N, Grose R. Fibroblast growth factor signalling: from development to cancer. Nat Rev Cancer 2010;10:116-29
11. Cappellen D, De Oliveira C, Ricol D, et al. Frequent activating mutations of FGFR3 in human bladder and cervix carcinomas. Nat Genet 1999;23:18-20
12. Knowles MA. Novel therapeutic targets in bladder cancer: mutation and expression of FGF receptors. Future Oncol 2008;4:71-83 (Pubitemid 351372608)
13. Dutt A, Salvesen HB, Chen TH, et al. Drug-sensitive FGFR2 mutations in endometrial carcinoma. Proc Natl Acad Sci USA 2008;105:8713-17 (Pubitemid 351987745)
14. Turner N, Pearson A, Sharpe R, et al. FGFR1 amplification drives endocrine therapy resistance and is a therapeutic target in breast cancer. Cancer Res 2010;70:2085-94
15. Casanovas O, Hicklin DJ, Bergers G, et al. Drug resistance by evasion of antiangiogenic targeting of VEGF signaling in late-stage pancreatic islet tumors. Cancer Cell 2005;8:299-309 (Pubitemid 41443415)
16. Bhide RS, Cai ZW, Zhang YZ, et al. Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol- 5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4] triazin-6-yloxy)propan-2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem 2006;49:2143-6
17. Cai ZW, Zhang Y, Borzilleri RM, et al. Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1Hindol- 5-yloxy)-5-methylpyrrolo[2,1-f] [1,2,4]triazin-6-yloxy)propan-2-yl)2- aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215). J Med Chem 2008;51:1976-80
18. Fargnoli J, Bhide R, Lombardo L, et al. Preclinical studies of BMS-582664, an alanine prodrug of BMS-540215, a potent, dual inhibitor of VEGFR-2 and FGFR-1 kinases [abstract 3033]. AACR Meeting Abstracts 2005
19. Shiang CY, Qi Y, Wang B, et al. Amplification of fibroblast growth factor receptor-1 in breast cancer and the effects of brivanib alaninate. Breast Cancer Res Treat 2010;123:747-55
20. Bhide RS, Lombardo LJ, Hunt JT, et al. The antiangiogenic activity in xenograft models of brivanib, a dual inhibitor of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinases. Mol Cancer Ther 2010;9:369-78
21. Ayers M, Dito G, Henley B, et al. Comparison of a dual inhibitor of VEGF and FGF signaling, BMS-582664, to the activity of bevacizumab, an inhibitor exclusively of VEGF signaling, in xenograft models of colon carcinoma [abstract 1618]. AACR Meeting Abstracts 2007
22. Poon RT, Ng IO, Lau C, et al. Correlation of serum basic fibroblast growth factor levels with clinicopathologic features and postoperative recurrence in hepatocellular carcinoma. Am J Surg 2001;182:298-304 (Pubitemid 32918381)
23. Huynh H, Ngo VC, Fargnoli J, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res 2008;14:6146-53
24. Rosen LS, Wilding G, Sweeney C, et al. Phase I dose escalation study to determine the safety, pharmacokinetics and pharmacodynamics of BMS-582664, a VEGFR/FGFR inhibitor in patients with advanced/metastatic solid tumors. J Clin Oncol 2006;24:abstract 3051
25. Garrett CR, Siu LL, El-Khoueiry AB, et al. A phase I study of brivanib alaninate (BMS-582664), an oral dual inhibitor of VEGFR and FGFR tyrosine kinases, in combination with full dose cetuximab (BC) in patients (pts) with advanced gastrointestinal malignancies (AGM) who failed prior therapy. J Clin Oncol 2008;26:abstract 4111
26. Investigator Brochure. Brivanib Alaninate/Brivanib (BMS-582664/ BMS-540215). Version date: 27-April-2010
27. Bristol-Myers Squibb. Ascending multiple-dose study of brivanib alaninate in combination with chemotherapeutic agents in subjects with advanced cancers. ClinicalTrials.gov NCT00798252. Available from: http://clinicaltrials.gov/ ct2/show/NCT00798252? term=NCT00798252&rank=1 [Last accessed 24 February 2011]
28. Lockhart AC, Rothenberg ML, Dupont J, et al. Phase I study of intravenous vascular endothelial growth factor trap, aflibercept, in patients with advanced solid tumors. J Clin Oncol 2010;28:207-14
29. Cheng HL. Dynamic contrast-enhanced MRI in oncology drug development. Curr Clin Pharmacol 2007;2:111-22
30. Malone H, Pictroski C, Kukral D, et al. Dynamic contrast enhanced magnetic resonance imaging (DCE-MRI) tumor microcirculation studies in tumor bearing mice treated with VEGFR inhibitor BMS-582664 [abstract 3869]. AACR Meeting Abstracts 2005
31. Bueno-de-Mesquita JM, Linn SC, Keijzer R, et al. Validation of 70-gene prognosis signature in node-negative breast cancer. Breast Cancer Res Treat 2009;117:483-95
32. Glinsky GV, Glinskii AB, Stephenson AJ, et al. Gene expression profiling predicts clinical outcome of prostate cancer. J Clin Invest 2004;113:913-23 (Pubitemid 38544150)
33. Glinsky GV. "Stemness" genomics law governs clinical behavior of human cancer: implications for decision making in disease management. J Clin Oncol 2008;26:2846-53
34. Ayers M, Fargnoli J, Lewin A, et al. Discovery and validation of biomarkers that respond to treatment with brivanib alaninate, a small-molecule VEGFR-2/ FGFR-1 antagonist. Cancer Res 2007;67:6899-906 (Pubitemid 47105537)
35. Jonker DJ, Rosen LS, Sawyer M, et al. A phase I study of BMS-582664 (brivanib alaninate), an oral dual inhibitor of VEGFR and FGFR tyrosine kinases, in patients (pts) with advanced/metastatic solid tumors: safety, pharmacokinetic (PK), and pharmacodynamic (PD) findings. J Clin Oncol 2007;25:abstract 3559
36. Platero S, Mokliatchouk O, Jayson GC, et al. Correlation of FGF2 tumor expression with tumor response, PFS, and changes in plasma pharmacodynamic (PD) markers following treatment with brivanib alaninate, an oral dual inhibitor of VEGFR and FGFR tyrosine kinases. J Clin Oncol 2008;26:abstract 3506
37. Marathe PH, Kamath AV, Zhang Y, et al. Preclinical pharmacokinetics and in vitro metabolism of brivanib (BMS-540215), a potent VEGFR2 inhibitor and its alanine ester prodrug brivanib alaninate. Cancer Chemother Pharmacol 2009;65:55-66
38. Hurwitz H, Lorusso P, Shapiro GI, et al. Phase 1 study of food effects on pharmacokinetics of brivanib alaninate in patients with advanced or metastatic solid tumors. Eur J Cancer 2008;6:abstract 429
39. Bristol-Myers Squibb. A Study of Brivanib (BMS-582664) in Patients With Liver Cancer and Mild, Moderate or Severe Liver Dysfunction. ClinicalTrials.gov NCT00437424. Available from: http://clinicaltrials.gov/ ct2/show/NCT00437424? term=NCT00437424&rank=1 [Last accessed 24 February 2011]
40. Nuyten DSA, Velasquez L, Garrett C, et al. Response assessment by CT and [18F] FDG-PET in a phase I study of brivanib, an oral selective dual inhibitor of FGF and VEGF signaling, in combination with cetuximab in patients with advanced gastrointestinal malignancies (AGM) [abstract 333]. Proceedings of the Gastrointestinal Cancers Symposium; 2009
41. Ayers M, Awad M, Malone D, et al. Correlation between K-ras status and efficacy results from a phase I/II study of brivanib alaninate in combination with cetuximab in patients (pts) with advanced or metastatic colorectal cancer (CRC) [abstract 375]. Proceedings of the Gastrointestinal Cancers Symposium; 2009
42. Bristol-Myers Squibb. Phase I/II Combination With Irinotecan- Erbitux. ClinicalTrials.gov NCT00594984. Available from: http://clinicaltrials.gov/ct2/ show/ NCT00594984?term=NCT00594984& rank=1 [Last accessed 24 February 2011]
43. Park YS, El-Khoueiry A, Cubillo A, et al. A blinded placebo (P) controlled phaseI/II dose escalation study (DES) of brivanib (B), an oral selective dual inhibitor of FGF and VEGF signaling, in combination with cetuximab (C) and irinotecan (I) in patients (pts) with KRAS wild type (KWT) advanced or metastatic colorectal cancer (AMCRC): Safety, tolerability and pharmacokinetic (PK) findings. Ann Oncol 2007;21(Suppl 8):abstract 614P
44. Bristol-Myers Squibb. Combination of Brivanib With 5-Fluorouracil/ Leucovorin (5FU/LV) and 5-Fluorouracil/ Leucovorin/Irinotecan (FOLFIRI). ClinicalTrials.gov NCT01046864. Available from: http://clinicaltrials.gov/ ct2/show/NCT01046864?term= NCT01046864&rank=1 [Last accessed 24 February 2011]
45. NCIC Clinical Trials Group. Cetuximab With or Without Brivanib in Treating Patients With Metastatic Colorectal Cancer. ClinicalTrials.gov NCT00640471. Available from: http:// clinicaltrials.gov/ct2/show/NCT00640471? term=NCT00640471&rank=1 [Last accessed 24 February 2011]
46. Raoul JL, Finn RS, Kang YK, et al. An open-label phase II study of first- and second-line treatment with brivanib in patients with hepatocellular carcinoma (HCC). J Clin Oncol 2009;27:abstract 4577
47. Finn RS, Raoul J-L, Manekas D, et al. An analysis of brivanib phase 2 data to investigate optimal assessment of treatment benefit with targeted agents for hepatocellular carcinoma (HCC) [abstract 0-031]. International Liver Cancer Association Annual Conference; 2010
48. Lencioni R, Llovet JM. Modified RECIST (mRECIST) assessment for hepatocellular carcinoma. Semin Liver Dis 2010;30:52-60
49. Bristol-Myers Squibb. First Line Hepato Cellular Carcinoma (HCC) ClinicalTrials.gov NCT00858871. Available from: http://clinicaltrials.gov/ ct2/show/NCT00858871?term= NCT00858871&rank=1 [Last accessed 24 February 2011]
50. Bristol-Myers Squibb. Comparison of Brivanib and Best Supportive Care to Placebo for Treatment of Liver Cancer for Those Subjects Who Have Failed Sorafenib Treatment. ClinicalTrials.gov NCT00825955. Available from: http://clinicaltrials.gov/ct2/show/ NCT00825955?term=NCT00825955& rank=1 [Last accessed 24 February 2011]
51. Bristol-Myers Squibb. Phase III Trans-Arterial Chemo-Embolization (TACE) Adjuvant HCC. ClinicalTrials. gov NCT00908752. Available from: http://clinicaltrials.gov/ct2/show/ NCT00908752?term=NCT00908752& rank=1 [Last accessed 24 February 2011]
52. Bristol-Myers Squibb. Ascending multiple-dose study of brivanib alaninate in combination with chemotherapeutic agents in subjects with advanced cancers. ClinicalTrials.gov NCT00798252. Available from: http://clinicaltrials.gov/ ct2/show/NCT00798252?term= NCT00798252&rank=1 [Last accessed 24 February 2011]
53. Bristol-Myers Squibb. Phase II study of brivanib (BMS-582664) to treat multiple tumor types. ClinicalTrials.gov NCT00633789. Available from: http://clinicaltrials.gov/ct2/show/ NCT00633789?term=NCT00633789& rank=1 [Last accessed 24 February 2011]
54. Gynecologic Oncology Group. Brivanib alaninate in treating patients with recurrent or persistent endometrial cancer. ClinicalTrials.gov NCT00888173. Available from: http://clinicaltrials.gov/ct2/show/ NCT00888173?term= NCT00888173& rank=1 [Last accessed 24 February 2011]
55. Roodink I, Leenders WP. Targeted therapies of cancer: angiogenesis inhibition seems not enough. Cancer Lett 2010;299:1-10