The invention relates generally to novel compounds of the auristatin family, to novel linkers for coupling a payload to another molecule, such a target-binding molecule, to novel linker-toxin molecules, and to novel antibody molecules that allow controlled, site-specific conjugation.

Improved processes for the preparation of tubulysin compounds, tubulysin drug linker compounds, and their intermediates are disclosed.

Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.

Provided are peptide analogs, pharmaceutical compositions comprising such compounds, and methods of treating cancer with such compounds.

The invention relates to a compound of formula (A) wherein n is an integer from 1 to 6, and R.sub.1, R.sub.1′, R.sub.2, R.sub.2′, R.sub.3, R.sub.3′ are cationic or hydrophobic residues.

##STR00001##

The invention relates to a compound of formula (A) wherein n is an integer from 1 to 6, and R.sub.1, R.sub.1′, R.sub.2, R.sub.2′, R.sub.3, R.sub.3′ are cationic or hydrophobic residues.

##STR00001##

The invention relates to platinum and rhenium complexes of formula (I) that may be used as imaging agents. In particular, the invention relates to imaging agents, for example imaging agents for use in the imaging of peroxisomes. Certain embodiments of the invention relate to compounds per se. Other embodiments relate to a process for the preparation of compounds and to the use of compounds as imaging agents. (Formula (I)) ##STR00001##

The present invention relates to a monoclonal antibody platform designed to be coupled to therapeutic peptides to increase the half-life of the therapeutic peptide in a subject. The invention also relates to pharmaceutical compositions and methods for use thereof.

Improved processes for the preparation of tubulysin compounds, tubulysin drug linker compounds, and their intermediates are disclosed.

The present disclosure provides for albumin-binding prodrugs of auristatin E derivatives and uses thereof.