Abstract: The present invention provides for new peptidic and peptidoid Bradykinin B1 receptor antagonists of formula (1) having good to excellent affinities and selectivity for the BKB1 receptor, and increased resistance to enzymatic degradation, superior pharmacokinetic properties, both in vitro and in vivo, with capability to significantly prevent and treat conditions wherein BKB1Rs are induced and over-expressed.

Abstract: The present invention relates to a method for the use of a bradykinin B1 receptor antagonist of formula I: X—CO-Aaa0-Aaa1-Aaa2-Aaa3-Gly-?(Me)Phe-Ser-D-?Nal-Aaa8-OH??(I) or a pharmaceutically acceptable salt or hydrate thereof wherein: X is CnH2n+1 or CiH2i—C6H5, where n is an integer from 1 to 3, and i is an integer from 0 to 3; Aaa0 is Lys, Orn or Cit; Aaa1 is Arg or Cit, and preferably Arg; Aaa2 is Oic, Hyp or Pro, and preferably Oic; Aaa3 is Pro or Oic, and preferably Pro; and Aaa8 is Ile, Leu, Nle, and preferably Ile, for the treatment of metastases, cancers and/or chemotherapy-induced neuropathies, comprising the administration of said compound to a patient in need of such treatment. The present invention also relates to compositions containing such antagonists and the uses thereof.