Abstract: Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.

Abstract: Shown and described are the synthesis of more potent forms of C-Mel, a prodrug used in Antibody-Directed Enzyme Prodrug Therapy, that releases the clinically used anticancer alkylating agent melphalan extracellularly. Shown and described are the synthesis of a variety of melphalan analogues with the intention to promote facile intracellular drug access. Esters, amides, and peptides of melphalan are shown. Cephalosporin prodrugs of the most interesting melphalan derivatives were synthesized and evaluated for potency, toxicity, therapeutic window, plasma stability, and solubility.

Abstract: The present invention relates to methods and compositions for the treatment of CD20-expressing cancers and immune disorders involving CD20-expressing cells. The present methods comprise administering to a subject an anti CD20 antibody-drug conjugate that has a high potency and/or is capable of internalizing into CD20-expressing cells. The present invention further provides pharmaceutical compositions and kits comprising such conjugates. The present invention yet further provides methods of and compositions relating to combination therapy of cancer and immune disorders involving CD20-expressing cells using the anti-CD20 antibody-drug conjugates of the invention.

Abstract: The present invention relates to methods for the treatment of immunological disorders other than cancer, comprising administering proteins characterized by their ability to bind to CD30 and exert a cytostatic or cytotoxic effect on an activated lymphocyte. Such proteins include monoclonal antibodies AC10 and IleFi1. AC10 and HeFi-1 derivatives, and antibodies that compete with AC10 and HeFi-1 for binding to CD30. Other such proteins include multivalent anti-CD30 antibodies and anti-CD30 antibodies conjugated to cytotoxic agents. Treatment modalities with antibodies of the invention are also provided.

Abstract: Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody, as disclosed.

Abstract: Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity. Prodrugs having targeting groups and pentapeptide moieities, as well as precursors thereof are also disclosed. For example, precursors having a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody, as disclosed.

Abstract: Pentapeptide compounds are disclosed. The compounds have biological activity, e.g., cytotoxicity, and/or include a reactive linker that can serve as a reaction site for joining to a targeting agent, e.g., an antibody.

Abstract: There are disclosed methods of use and pharmaceutical compositions for two related genera of low molecular weight compounds comprising optionally substituted iminoquinone or orthoquinone ring systems. The compounds have MIF (macrophage migration inhibitory factor) antagonist activity and find utility as such. For example, the compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases (including rheumatiod arthritis, insulin-dependent diabetes, multiple sclerosis, graft versus host disease, lupus syndromes), asthma, arthritis, EAE, ARDS, psoriasis, interleukin-2 toxicity, proliferative vascular disease, and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization (angiogenesis).