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Chemical Compound Review

Livostin     (3R,4R)-1-[4-cyano-4-(4...

Synonyms: Bilina, Levocabastin, Levocabastina, Levocobastine, levocabastine, ...
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Disease relevance of levocabastine

  • BACKGROUND: Multiple ocular challenges or seasonal trials have demonstrated the efficacy of levocabastine and nedocromil sodium in the treatment of allergic conjunctivitis [1].
  • Results showed that levocabastine was significantly more effective than placebo in inhibiting itching, hyperemia, eyelid swelling, chemosis, and tearing after the initial challenge and in inhibiting all parameters except eyelid swelling after the rechallenge 4 hours later (p < 0.05) [2].
  • A late allergic reaction was observed by the patient in 6/11 CPTs performed after placebo treatment and 8/11 after levocabastine treatment [3].
  • Conjunctival itching (symptom score) and erythema (percent conjunctival surface) were also better controlled by levocabastine than by nedocromil during provocation (p < 0.05) [1].
  • However, the results available to date suggest that the topical formulations of levocabastine are a valuable treatment option in patients with allergic rhinitis and/or conjunctivitis [4].

Psychiatry related information on levocabastine


High impact information on levocabastine


Chemical compound and disease context of levocabastine


Biological context of levocabastine


Anatomical context of levocabastine

  • The pharmacological properties of this receptor correspond to those of the low-affinity, levocabastine-sensitive NT binding site described initially in membranes prepared from rat and mouse brain [7].
  • After a preliminary provocation to determine conjunctival reaction threshold (erythema of at least 50% of the conjunctiva with ocular itching), patients were randomized to receive either topical levocabastine (0.05%) or nedocromil (2%) 15 minutes before provocation [1].
  • Nedocromil sodium reduced mast cell function, whereas levocabastine appeared to have primarily antihistaminic actions, although it also reduced the expression of intercellular adhesion molecule 1 [19].
  • The latter phenomenon may be due, at least in part, to a direct effect of levocabastine on epithelial cells [20].
  • CONCLUSION: Levocabastine exerts anti-allergic activity, in that it reduces in vivo inflammatory cell infiltration due to ASCC, and also adhesion molecule expression on conjunctival epithelium [20].

Associations of levocabastine with other chemical compounds

  • Visual analogue scale ratings in patients' diaries indicated that at the end of therapy, nasal symptoms were less severe in the levocabastine-treated group than in the sodium cromoglycate-treated (p = 0.03) or placebo-treated group (p = 0.001) [21].
  • BACKGROUND: This study was designed to compare the efficacy and tolerability of a new topical (nasal spray and eye drops) H1-receptor antagonist, levocabastine, with that of orally administered terfenadine for the prophylaxis and treatment of seasonal allergic rhinoconjunctivitis [22].
  • Potent histamine H1-receptor antagonists (e.g. azelastine and levocabastine) are approved for local treatment and lead to prompt relief of troublesome symptoms [23].
  • Colonic responses to NT in both segments were virtually the same in the presence of atropine (1 microm), levocabastine (10 microM) or tetrodotoxin (1 microM) [24].
  • Leukocytes obtained from allergic volunteers were preincubated for 30 minutes with levocabastine (doses 10(-8) M to 10(-6) M) and thereafter incubated with allergen [25].

Gene context of levocabastine


Analytical, diagnostic and therapeutic context of levocabastine


  1. Comparison of effects of topical levocabastine and nedocromil sodium on the early response in a conjunctival provocation test with allergen. Hammann, C., Kämmerer, R., Gerber, M., Spertini, F. J. Allergy Clin. Immunol. (1996) [Pubmed]
  2. Evaluation of the new ophthalmic antihistamine, 0.05% levocabastine, in the clinical allergen challenge model of allergic conjunctivitis. Abelson, M.B., George, M.A., Schaefer, K., Smith, L.M. J. Allergy Clin. Immunol. (1994) [Pubmed]
  3. Effect of levocabastine, a new H1 antagonist, in a conjunctival provocation test with allergens. Zuber, P., Pécoud, A. J. Allergy Clin. Immunol. (1988) [Pubmed]
  4. Levocabastine. An update of its pharmacology, clinical efficacy and tolerability in the topical treatment of allergic rhinitis and conjunctivitis. Noble, S., McTavish, D. Drugs (1995) [Pubmed]
  5. Central effect of the potent long-acting H1-antihistamine levocabastine. Tasaka, K., Kamei, C., Tsujimoto, S., Yoshida, T., Aoki, I. Arzneimittel-Forschung. (1990) [Pubmed]
  6. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Gully, D., Canton, M., Boigegrain, R., Jeanjean, F., Molimard, J.C., Poncelet, M., Gueudet, C., Heaulme, M., Leyris, R., Brouard, A. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
  7. Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain. Mazella, J., Botto, J.M., Guillemare, E., Coppola, T., Sarret, P., Vincent, J.P. J. Neurosci. (1996) [Pubmed]
  8. Identification and functional characterization of a 5-transmembrane domain variant isoform of the NTS2 neurotensin receptor in rat central nervous system. Perron, A., Sarret, P., Gendron, L., Stroh, T., Beaudet, A. J. Biol. Chem. (2005) [Pubmed]
  9. Recycling ability of the mouse and the human neurotensin type 2 receptors depends on a single tyrosine residue. Martin, S., Vincent, J.P., Mazella, J. J. Cell. Sci. (2002) [Pubmed]
  10. Intranasal azelastine. A review of its efficacy in the management of allergic rhinitis. McNeely, W., Wiseman, L.R. Drugs (1998) [Pubmed]
  11. Levocabastine. Evaluation in the histamine and compound 48/80 models of ocular allergy in humans. Abelson, M.B., Smith, L.M. Ophthalmology (1988) [Pubmed]
  12. Double-blind comparison of levocabastine eye drops with sodium cromoglycate and placebo in the treatment of seasonal allergic conjunctivitis. Azevedo, M., Castel-Branco, M.G., Oliveira, J.F., Ramos, E., Delgado, L., Almeida, J. Clin. Exp. Allergy (1991) [Pubmed]
  13. Evaluation of 0.05% levocabastine versus 4% sodium cromolyn in the allergen challenge model. Abelson, M.B., George, M.A., Smith, L.M. Ophthalmology (1995) [Pubmed]
  14. Levocabastine: an effective topical treatment of allergic rhinoconjunctivitis. Janssens, M.M., Vanden Bussche, G. Clin. Exp. Allergy (1991) [Pubmed]
  15. Pharmacokinetics of orally administered levocabastine in patients with renal insufficiency. Zazgornik, J., Huang, M.L., Van Peer, A., Woestenborghs, R., Heykants, J., Stephen, A. Journal of clinical pharmacology. (1993) [Pubmed]
  16. Reversal of histamine-induced bronchoconstriction by the H1-receptor antagonist levocabastine: a potential model for efficacy in anaphylaxis. Ferner, R.E., Ward, C., Kelly, C., Connolly, M., Bateman, D.N., Rawlins, M.D. British journal of clinical pharmacology. (1988) [Pubmed]
  17. Two populations of neurotensin binding sites in murine brain: discrimination by the antihistamine levocabastine reveals markedly different radioautographic distribution. Kitabgi, P., Rostène, W., Dussaillant, M., Schotte, A., Laduron, P.M., Vincent, J.P. Eur. J. Pharmacol. (1987) [Pubmed]
  18. Influence of levocabastine suspension on ciliary beat frequency and mucociliary clearance. Merkus, F.W., Schüsler-van Hees, M.T. Allergy (1992) [Pubmed]
  19. Nedocromil sodium and levocabastine reduce the symptoms of conjunctival allergen challenge by different mechanisms. Ahluwalia, P., Anderson, D.F., Wilson, S.J., McGill, J.I., Church, M.K. J. Allergy Clin. Immunol. (2001) [Pubmed]
  20. Topical ocular levocabastine reduces ICAM-1 expression on epithelial cells both in vivo and in vitro. Buscaglia, S., Paolieri, F., Catrullo, A., Fiorino, N., Riccio, A.M., Pesce, G., Montagna, P., Bagnasco, M., Ciprandi, G., Canonica, G.W. Clin. Exp. Allergy (1996) [Pubmed]
  21. Levocabastine nasal spray better than sodium cromoglycate and placebo in the topical treatment of seasonal allergic rhinitis. Schata, M., Jorde, W., Richarz-Barthauer, U. J. Allergy Clin. Immunol. (1991) [Pubmed]
  22. Topical levocabastine compared with orally administered terfenadine for the prophylaxis and treatment of seasonal rhinoconjunctivitis. Søhoel, P., Freng, B.A., Kramer, J., Poppe, S., Rebo, R., Korsrud, F.R., Garud, O., Woxen, O.J., Olsen, A.K. J. Allergy Clin. Immunol. (1993) [Pubmed]
  23. Seasonal allergic rhinitis. Newer treatment approaches. Horak, F. Drugs (1993) [Pubmed]
  24. In vitro functional evidence of different neurotensin-receptors modulating the motor response of human colonic muscle strips. Croci, T., Aureggi, G., Guagnini, F., Manara, L., Gully, D., Fur, G.L., Maffrand, J.P., Mukenge, S., Ferla, G., Ferrara, P., Chalon, P., Vita, N. Br. J. Pharmacol. (1999) [Pubmed]
  25. Selective effect of levocabastine on histamine receptor and histamine release from human leukocytes and guinea pig isolated tissue. Garrelds, I.M., de Graaf-in't Veld, T., van Toorenenbergen, A.W., van Wijk, R.G., Boegheim, J.P., Saxena, P.R., Zijlstra, F.J. Ann. Allergy Asthma Immunol. (1996) [Pubmed]
  26. Regional and cellular distribution of low affinity neurotensin receptor mRNA in adult and developing mouse brain. Sarret, P., Beaudet, A., Vincent, J.P., Mazella, J. J. Comp. Neurol. (1998) [Pubmed]
  27. Effects of topical treatment with H1 and H2 antagonists on clinical symptoms and nasal vascular reactions in patients with allergic rhinitis. Holmberg, K., Pipkorn, U., Bake, B., Blychert, L.O. Allergy (1989) [Pubmed]
  28. Preferential inhibition of human phosphodiesterase 4 by ibudilast. Huang, Z., Liu, S., Zhang, L., Salem, M., Greig, G.M., Chi Chung Chan, n.u.l.l., Natsumeda, Y., Noguchi, K. Life Sci. (2006) [Pubmed]
  29. Levocabastine. A review of its pharmacological properties and therapeutic potential as a topical antihistamine in allergic rhinitis and conjunctivitis. Dechant, K.L., Goa, K.L. Drugs (1991) [Pubmed]
  30. Molecular cloning of a levocabastine-sensitive neurotensin binding site. Chalon, P., Vita, N., Kaghad, M., Guillemot, M., Bonnin, J., Delpech, B., Le Fur, G., Ferrara, P., Caput, D. FEBS Lett. (1996) [Pubmed]
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