University of California

Manzanita Pharmaceuticals, Inc.

Asilomar Pharmaceuticals, Inc.

Stephen B Kahl

Constance A McKee

Myoung-Seo Koo

Robert R Webb

G Craig Hill

Gordon Craig Hill

Conjugates for delivering an anti-cancer agent to nerve cells are provided. Conjugate compounds of the present disclosure according to certain embodiments include a compound having a protein, peptide or pepetidomimetic that binds selectively to a neurotrophin receptor, an anti-cancer agent and a linker that covalently bonds the anti-cancer agent to the protein, peptide or pepetidomimetic binds selectively to the neurotrophin receptor. Compositions and methods for delivering an anti-cancer agent selectively into nerve cells (e.g., in the treatment of optic pathway glioma) as well as indications such as perineural invasion and skin cancers are also described. Also provided are methods of making the anti-cancer conjugate compounds.

Conjugates for delivering an anti-cancer agent to nerve cells, methods of use and methods of making thereof

The invention features compounds of the general formula:B-L-Mwhere B is a binding agent capable of selectively binding to a nerve cell surface receptor and mediating absorption of the compound by the nerve cell; M is a moiety which performs a useful non-cytotoxic function when absorbed by a nerve cell, and can be a therapeutic moiety or an imaging moiety; and L is a linker coupling B to M. The invention also features methods of use of the compounds in, for example, treating conditions such as viral infections and pain, as well as in labeling nerve cells.

Compounds for delivery of therapeutic and imaging moieties to nerve cells

A method for improving intracellular administration of a therapeutic agent is provided comprising: contacting cells with a compound comprising a charged derivative of a therapeutic agent having a therapeutic activity, the charged derivative being conjugated to a protein having a biological activity of being transported across a cell membrane into a cell; and having the cell transport the compound into the cell where the cell metabolizes at least a portion of the compound to form a charged metabolite product that possesses the therapeutic activity of the therapeutic agent, the charged metabolite product being less prone to being transported across the cell membrane out of the cell relative to the compound and less prone to being transported across the cell membrane out of the cell relative to the therapeutic agent.

Compounds for intracellular delivery of therapeutic moieties to nerve cells

Carborane substituted porphyrin compounds complexed with a metal or transition metal have a variety of therapeutic uses. These compounds have been found, for example, selectively to inhibit viral aspartyl proteases. The transition metal complexes are useful both therapeutically in BNCT (boron neutron capture therapy) as well as for MR contrast enhancement. Particularly preferred compounds in accordance with the invention use the dipotassium salt of 2,4-bis-[.alpha.,.beta.-(1,2-dicarbaclosododecaborane carboxy)ethyl]deuteroporphyrin, which is complexed with a metal or a transition metal. These compounds are well solubilized in water, and are suitable for oral administration.

Boronated metalloporphyrine and therapeutic methods

Drug delivery porphyrin compositions and methods

A compound is described having the structure ##STR1## where R preferably is ##STR2## and most preferably R.sup.3 is a closo-carborane and R.sup.2 is --H, an alkyl or aryl having 1 to about 7 carbon atoms,

Growing community of inventors

Portola Valley, CA, United States of America

Stephen B Kahl