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Chemical Compound Review

Vapreotida     10-(4-aminobutyl)-N-[1- aminocarbonyl-2-(1H...

Synonyms: Vapreotide, Vapreotidum, CCRIS 6495, RC-160, AC1L2FXK, ...
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Disease relevance of Sanvar IR


High impact information on Sanvar IR

  • METHODS: We studied the effects of treatment with vapreotide, a somatostatin analogue, begun before endoscopic treatment in 227 patients with cirrhosis who were hospitalized for acute upper gastrointestinal bleeding [1].
  • The ability of the carriers and the hybrids to inhibit the binding of 125I-labeled RC-160 to receptors for SST on rat pituitary membrane preparation was also determined [6].
  • In H-345 human small cell lung carcinoma cell line, conjugates of RC-121 preserved the cytotoxic activity of their radicals, but the hybrids with RC-160 showed approximately 10 times lower activity [6].
  • RC-160 inhibited both CCK-induced intracellular cGMP formation as well as activation of p42-MAP kinase phosphorylation and activity [7].
  • These effects are positively regulated by CCK and negatively influenced by RC-160, interacting through CCKA and sst5 receptors, respectively [7].

Chemical compound and disease context of Sanvar IR


Biological context of Sanvar IR

  • A good correlation between the affinities of RC-160 and SMS-201-995 for each receptor subtype and their potencies to inhibit cell proliferation suggests the involvement of these receptors in cell growth regulation [13].
  • Examinations of HT-29, A-549, and R3230AC cancer cell lines revealed no phosphorylation by EGF or dephosphorylation by RC-160 and [D-Trp6]LH-RH [14].
  • This shows that phosphorylation regulates binding of LH-RH and may explain the up-regulation by EGF and down-regulation by RC-160 and by LH-RH of the LH-RH response [15].
  • Binding experiments were performed on crude membranes by using [125I-labeled Tyr11] somatostatin-14; RC-160 exhibited moderate-to-high affinities for SSTR2, -3, and -5 (IC50, 0.17, 0.1 and 21 nM, respectively) and low affinity for SSTR1 and -4 (IC50, 200 and 620 nM, respectively) [16].
  • In studies in vitro, RC-3095, added to the culture medium, significantly inhibited the proliferation of U-87MG and U-373MG cells in the presence of GRP(14-27), as measured by cell number, but only a moderate suppression of growth of both cell lines was observed with somatostatin analogue RC-160 [17].

Anatomical context of Sanvar IR

  • In the second experiment, 3-mm3 fragments of Dunning R-3327-AT-1 tumor were implanted orthotopically into the prostates of Copenhagen rats in order to evaluate the survival time of animals bearing this cancer during treatment with RC-160 released from Alzet osmotic minipumps at a dose of 100 micrograms/day/rat [4].
  • RC-160 and somatuline displaced radiolabel from binding sites in gastric and colonic cancer and mucosa with 10-fold lower affinity than the native peptide [18].
  • We also investigated the effect of RC-160 microcapsules on hyperprolactinemic female rats implanted with pituitary glands under the kidney capsules [19].
  • Both LH-RH antagonist SB-75 and somatostatin analog RC-160 caused a significant inhibition of tumors, and their combination had the strongest tumor inhibitory effect, with the best survival of animals, the lowest tumorous pancreas weight and the highest apoptosis index among groups [20].
  • In the present study we investigated the effects of the somatostatin (SS) analogs octreotide, RC-160, and BIM-23014 on GH release by cultured cells of human GH-secreting pituitary tumors, in normal rat anterior pituitary cells, and on gastrin release by cultured cells from a human gastrinoma [9].

Associations of Sanvar IR with other chemical compounds


Gene context of Sanvar IR


Analytical, diagnostic and therapeutic context of Sanvar IR

  • The patients in the vapreotide group received significantly fewer blood transfusions (2.0+/-2.2 vs. 2.8+/-2.8 units, P=0.04) [1].
  • RESULTS: At the time of endoscopy, active bleeding was evident in 28 of 91 patients in the vapreotide group (31 percent), as compared with 43 of 93 patients in the placebo group (46 percent) (P=0.03) [1].
  • The most striking decrease in tumor weight and volume was obtained in animals treated with microcapsules of [D-Trp6]LH-RH combined with the delayed delivery system for RC-160 [26].
  • Twelve weeks after treatment, fluorescence had decreased significantly among animals treated for 2 weeks with RC-3095 (control, 0.53 +/- 0.03 V vs. RC-3095, 0.28 +/- 0.03 V; P < 0.0005) or with RC-160 (control, 0.85 +/- 0.03 V vs. RC-160, 0.24 +/- 0.03 V; P < 0.0001) [3].
  • A sensitive and specific radioimmunoassay (RIA) for RC-160 was developed and used for following the rate of liberation of this peptide from microcapsules of poly(DL-lactide-coglycolide) [27].


  1. Early administration of vapreotide for variceal bleeding in patients with cirrhosis. Calès, P., Masliah, C., Bernard, B., Garnier, P.P., Silvain, C., Szostak-Talbodec, N., Bronowicki, J.P., Ribard, D., Botta-Fridlund, D., Hillon, P., Besseghir, K., Lebrec, D. N. Engl. J. Med. (2001) [Pubmed]
  2. Somatostatin analogues inhibit growth of pancreatic cancer by stimulating tyrosine phosphatase. Liebow, C., Reilly, C., Serrano, M., Schally, A.V. Proc. Natl. Acad. Sci. U.S.A. (1989) [Pubmed]
  3. Peptide analogues alter the progression of premalignant lesions, as measured by Photofrin fluorescence. Liebow, C., Crean, D.H., Schally, A.V., Mang, T.S. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
  4. Inhibitory effects of somatostatin analogue RC-160 and bombesin/gastrin-releasing peptide antagonist RC-3095 on the growth of the androgen-independent Dunning R-3327-AT-1 rat prostate cancer. Pinski, J., Reile, H., Halmos, G., Groot, K., Schally, A.V. Cancer Res. (1994) [Pubmed]
  5. Inhibitory effect of somatostatin analogue RC-160 on the growth of hepatic metastases of colon cancer in rats: a study with magnetic resonance imaging. Qin, Y., Van Cauteren, M., Osteaux, M., Schally, A.V., Willems, G. Cancer Res. (1992) [Pubmed]
  6. Synthesis and biological evaluation of cytotoxic analogs of somatostatin containing doxorubicin or its intensely potent derivative, 2-pyrrolinodoxorubicin. Nagy, A., Schally, A.V., Halmos, G., Armatis, P., Cai, R.Z., Csernus, V., Kovács, M., Koppán, M., Szepesházi, K., Kahán, Z. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  7. Characterization of the antiproliferative signal mediated by the somatostatin receptor subtype sst5. Cordelier, P., Estève, J.P., Bousquet, C., Delesque, N., O'Carroll, A.M., Schally, A.V., Vaysse, N., Susini, C., Buscail, L. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  8. Expression of somatostatin receptors in uveal melanomas. Ardjomand, N., Ardjomand, N., Schaffler, G., Radner, H., El-Shabrawi, Y. Invest. Ophthalmol. Vis. Sci. (2003) [Pubmed]
  9. Relative potencies of the somatostatin analogs octreotide, BIM-23014, and RC-160 on the inhibition of hormone release by cultured human endocrine tumor cells and normal rat anterior pituitary cells. Hofland, L.J., van Koetsveld, P.M., Waaijers, M., Zuyderwijk, J., Lamberts, S.W. Endocrinology (1994) [Pubmed]
  10. Somatostatin analog RC-160 inhibits the growth of human osteosarcomas in nude mice. Pinski, J., Schally, A.V., Halmos, G., Szepeshazi, K., Groot, K. Int. J. Cancer (1996) [Pubmed]
  11. Histologic changes in the rat prostate cancer model after treatment with somatostatin analogs and D-Trp-6-LH-RH. Zalatnai, A., Paz-Bouza, J.I., Redding, T.W., Schally, A.V. Prostate (1988) [Pubmed]
  12. Effect of microcapsules of luteinizing hormone-releasing hormone antagonist SB-75 and somatostatin analog RC-160 on endocrine status and tumor growth in the Dunning R-3327H rat prostate cancer model. Yano, T., Pinski, J., Szepeshazi, K., Milovanovic, S.R., Groot, K., Schally, A.V. Prostate (1992) [Pubmed]
  13. Stimulation of tyrosine phosphatase and inhibition of cell proliferation by somatostatin analogues: mediation by human somatostatin receptor subtypes SSTR1 and SSTR2. Buscail, L., Delesque, N., Estève, J.P., Saint-Laurent, N., Prats, H., Clerc, P., Robberecht, P., Bell, G.I., Liebow, C., Schally, A.V. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  14. Effects of epidermal growth factor and analogues of luteinizing hormone-releasing hormone and somatostatin on phosphorylation and dephosphorylation of tyrosine residues of specific protein substrates in various tumors. Lee, M.T., Liebow, C., Kamer, A.R., Schally, A.V. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
  15. Regulation of luteinizing hormone-releasing hormone receptor binding by heterologous and autologous receptor-stimulated tyrosine phosphorylation. Liebow, C., Lee, M.T., Kamer, A.R., Schally, A.V. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
  16. Inhibition of cell proliferation by the somatostatin analogue RC-160 is mediated by somatostatin receptor subtypes SSTR2 and SSTR5 through different mechanisms. Buscail, L., Estève, J.P., Saint-Laurent, N., Bertrand, V., Reisine, T., O'Carroll, A.M., Bell, G.I., Schally, A.V., Vaysse, N., Susini, C. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  17. Somatostatin analogues and bombesin/gastrin-releasing peptide antagonist RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. Pinski, J., Schally, A.V., Halmos, G., Szepeshazi, K., Groot, K. Cancer Res. (1994) [Pubmed]
  18. Somatostatin binding in human gastrointestinal tissues: effect of cations and somatostatin analogues. Miller, G.V., Preston, S.R., Woodhouse, L.F., Farmery, S.M., Primrose, J.N. Gut (1993) [Pubmed]
  19. Delayed release formulation of the somatostatin analog RC-160 inhibits the growth hormone (GH) response to GH-releasing factor-(1-29)NH2 and decreases elevated prolactin levels in rats. Bokser, L., Schally, A.V. Endocrinology (1988) [Pubmed]
  20. Effect of combination treatment with analogs of luteinizing hormone-releasing hormone (LH-RH) or somatostatin and 5-fluorouracil on pancreatic cancer in hamsters. Szepeshazi, K., Lapis, K., Schally, A.V. Int. J. Cancer (1991) [Pubmed]
  21. Rhenium-labeled somatostatin analog RC-160. 1H NMR and computer modeling conformational analysis. Varnum, J.M., Thakur, M.L., Schally, A.V., Jansen, S., Mayo, K.H. J. Biol. Chem. (1994) [Pubmed]
  22. sst2 Somatostatin receptor inhibits cell proliferation through Ras-, Rap1-, and B-Raf-dependent ERK2 activation. Lahlou, H., Saint-Laurent, N., Estève, J.P., Eychène, A., Pradayrol, L., Pyronnet, S., Susini, C. J. Biol. Chem. (2003) [Pubmed]
  23. High expression of somatostatin receptors and messenger ribonucleic acid for its receptor subtypes in organ-confined and locally advanced human prostate cancers. Halmos, G., Schally, A.V., Sun, B., Davis, R., Bostwick, D.G., Plonowski, A. J. Clin. Endocrinol. Metab. (2000) [Pubmed]
  24. Somatostatin analogs for diagnosis and treatment of cancer. Weckbecker, G., Raulf, F., Stolz, B., Bruns, C. Pharmacol. Ther. (1993) [Pubmed]
  25. Antagonists of growth hormone-releasing hormone and somatostatin analog RC-160 inhibit the growth of the OV-1063 human epithelial ovarian cancer cell line xenografted into nude mice. Chatzistamou, I., Schally, A.V., Varga, J.L., Groot, K., Armatis, P., Busto, R., Halmos, G. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  26. Somatostatin analogs as adjuncts to agonists of luteinizing hormone-releasing hormone in the treatment of experimental prostate cancer. Schally, A.V., Redding, T.W. Proc. Natl. Acad. Sci. U.S.A. (1987) [Pubmed]
  27. Radioimmunoassay for octapeptide analogs of somatostatin: measurement of serum levels after administration of long-acting microcapsule formulations. Mason-Garcia, M., Vaccarella, M., Horvath, J., Redding, T.W., Groot, K., Orsolini, P., Schally, A.V. Proc. Natl. Acad. Sci. U.S.A. (1988) [Pubmed]
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