Abstract: The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer.

Abstract: The present application relates to methods and uses of conjugates comprising antitumor agents (e.g., chemotherapeutic agents) conjugated to peptide compounds targeting Sortilin-expressing cancer stem cells (CSCs), in embodiments for the treatment of poor prognosis cancers refractory to standard antitumor therapies associated the presence of Sortilin-expressing CSCs, and for preventing or treating cancer relapse or recurrence.

Abstract: The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer.

Abstract: The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer and increasing cellular internalization of said peptide compounds. The peptide compounds are selected from the following group consisting of; GVRAKAGVRNMFKSESY as set forth in SEQ ID NO: 9; GVRAKAGVRN(Nle)FKSESY as set forth in SEQ ID NO: 10; and YKSLRRKAPRWDAPLRDPALRQLL as set forth in SEQ ID NO: 11; and wherein at least one protecting group and/or at least one labelling agent is connected to said peptide compound.

Abstract: The present invention features a compound having the formula A-X-B, where A is peptide vector capable of enhancing transport of the compound across the blood-brain barrier or into particular cell types, X is a linker, and B is a peptide therapeutic selected from the group consisting of neurotensin, a neurotensin analog, or a neurotensin receptor agonist. The compounds of the invention can be used to treat any disease in which increased neurotensin activity is useful and can be used to induce hypothermia or analgesia.

Abstract: The present invention relates to short polypeptides (e.g., fewer than 19 amino acids in length) and longer polypeptides (e.g., 19 or more amino acids in length) having one or more D-amino acids as targeting moieties. These polypeptides, when conjugated to agents (e.g., therapeutic agents or transport vectors) are capable of transporting the agents across the BBB or into particular cell types. In particular, the short polypeptides can include one or more D-amino acids. These compounds are therefore particularly useful in the treatment of neurological diseases or diseases associated with particular cell types, organs, or tissues.

Abstract: The present invention relates to antibody-polypeptide-cytotoxin conjugates and methods of making, packaging, and using the conjugates. The polypeptide can be a Kunitz-type protease inhibitor or a derivative thereof that facilitates transport of the conjugate across the blood-brain barrier and/or into cancer cells outside the CNS, and the antibody moiety selectively binds a target within the CNS or in peripheral tumors to direct the cytotoxic agent to that target (e.g., a tumor or cancer cell). The conjugates can be further defined by the inclusion of a linker between the antibody moiety and the polypeptide; by the number of polypeptides and cytotoxic agents conjugated thereto; by the positions at which the entities within the conjugates are bound to one another; and by the larger configuration of the conjugate. Modified polypeptides (e.g., polypeptides conjugated to cytotoxic agents but not to an anti-body moiety), pharmaceutical compositions, kits (e.g.

Abstract: The present invention relates to antibody-polypeptide-cytotoxin conjugates and methods of making, packaging, and using the conjugates. The polypeptide can be a Kunitz-type protease inhibitor or a derivative thereof that facilitates transport of the conjugate across the blood-brain barrier and/or into cancer cells outside the CNS, and the antibody moiety selectively binds a target within the CNS or in peripheral tumors to direct the cytotoxic agent to that target (e.g., a tumor or cancer cell). The conjugates can be further defined by the inclusion of a linker between the antibody moiety and the polypeptide; by the number of polypeptides and cytotoxic agents conjugated thereto; by the positions at which the entities within the conjugates are bound to one another; and by the larger configuration of the conjugate. Modified polypeptides (e.g., polypeptides conjugated to cytotoxic agents but not to an antibody moiety), pharmaceutical compositions, kits (e.g.

Abstract: The present invention relates to carriers, conjugate and pharmaceutical compositions and their use to increase the potency of drugs and to modify the pharmacokinetics of compounds. More particularly, the present invention relates to conjugates comprising the carrier described herein and their use in the treatment and diagnostic of cancer.

Abstract: The invention relates to dendrimers conjugated to multiple targeting peptides and one or more therapeutic, diagnostic, or imaging agents for delivery of such agents across the blood-brain barrier and into certain cell types including, cells expressing the LRP-1 receptor. Also described are methods of making compounds that comprise dendrimers conjugated to targeting peptides and therapeutic, diagnostic, or imaging agents.

Abstract: The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptide derived from aprotinin and from aprotinin analogs as well as conjugates and pharmaceutical compositions comprising these polypeptides. The present invention also relates to the use of these polypeptide for transporting an antibody or antibody fragment across the blood-brain barrier of an individual and in the treatment and diagnosis of neurological diseases.

Abstract: The present invention relates to short polypeptides (e.g., fewer than 19 amino acids in length) and longer polypeptides (e.g., 19 or more amino acids in length) having one or more D-amino acids as targeting moieties. These polypeptides, when conjugated to agents (e.g., therapeutic agents or transport vectors) are capable of transporting the agents across the BBB or into particular cell types. In particular, the short polypeptides can include one or more D-amino acids. These compounds are therefore particularly useful in the treatment of neurological diseases or diseases associated with particular cell types, organs, or tissues.

Abstract: The present invention relates to protein conjugates comprising an aprotinin-derived polypeptide, which facilitates transport of the conjugate across the blood-brain barrier, and an antibody moiety that selectively binds a target within the CNS. The protein conjugates are further defined by the inclusion of a linker; by the number of polypeptides conjugated to each antibody moiety; by the positions at which the antibody moiety and the polypeptides are conjugated; and by the larger configuration of the conjugate (in which every polypeptide is linked only to the antibody moiety). Modified aprotinin-derived polypeptides, linker-bound antibody moieties, pharmaceutical compositions, kits, and methods of making and using the protein conjugates are also features of the invention.

Abstract: Based on our identification of a polypeptide (Angiopep-7) that is efficiently transported to cells such as liver, lung, kidney, spleen, and muscle, the invention provides polypeptides, conjugates including the polypeptides, and methods for treating diseases associated with these cell types. Unlike other aprotinin related polypeptides identified herein (including Angiopep-3, Angiopep-4a Angiopep-4b Angiopep-5, and Angiopep-6) which efficiently cross the blood-brain barrier (BBB), Angiopep-7 is not efficiently transported across the BBB.

Abstract: The present invention relates to antibody-polypeptide-cytotoxin conjugates and methods of making, packaging, and using the conjugates. The polypeptide can be a Kunitz-type protease inhibitor or a derivative thereof that facilitates transport of the conjugate across the blood-brain barrier and/or into cancer cells outside the CNS, and the antibody moiety selectively binds a target within the CNS or in peripheral tumors to direct the cytotoxic agent to that target (e.g., a tumor or cancer cell). The conjugates can be further defined by the inclusion of a linker between the antibody moiety and the polypeptide; by the number of polypeptides and cytotoxic agents conjugated thereto; by the positions at which the entities within the conjugates are bound to one another; and by the larger configuration of the conjugate. Modified polypeptides (e.g., polypeptides conjugated to cytotoxic agents but not to an antibody moiety), pharmaceutical compositions, kits (e.g.

Abstract: The present invention relates to improvements in the field of drug delivery. More particularly, the invention relates to a non-invasive and flexible method and carrier for transporting a compound or drug across the blood-brain barrier of an individual. In particular the present invention relates to a carrier for transporting an agent attached thereto across a blood-brain barrier, wherein the carrier is able to cross the blood-brain barrier after attachment to the agent and thereby transport the agent across the blood-brain barrier. The present invention relates to improvements in the field of drug delivery. More particularly, the invention relates to a non-invasive and flexible method and carrier for transporting a compound or drug across the blood-brain barrier of an individual.

Abstract: The present invention relates to carriers, conjugate and pharmaceutical compositions and their use to increase the potency of drugs and to modify the pharmacokinetics of compounds. More particularly, the present invention relates to conjugates comprising the carrier described herein and their use in the treatment and diagnostic of cancer.

Abstract: Ovarian cancer is treated with conjugates of an anticancer agent and an Angiopep-2 polypeptide analog (i.e. a polypeptide comprising an amino acid sequence at least 80% identical to Seq. ID NO:97). Such treatment includes utility in treating metastatic ovarian cancer and in treating patients who have previously exhibited resistance to standard chemotherapeutic agents. Preferred anticancer agents include taxanes while the preferred conjugate is ANG1005, a conjugate comprising three molecules of paclitaxel conjugated to the peptide Angiopep-2.

Abstract: The present invention relates to multimeric (e.g., dimeric, trimeric) forms of peptide vectors that are capable of crossing the blood-brain barrier (BBB) or efficiently entering particular cell types. These multimeric peptide vectors, when conjugated to agents (e.g., therapeutic agents) are capable of transporting the agents across the BBB or into particular cell types. These compounds are therefore particularly useful in the treatment of neurological diseases.

Abstract: The present invention is related to a compound that includes a lysosomal enzyme and a targeting moiety, for example, a compound that includes iduronate-2-sulfatase conjugated to Angiopep-2 through a linker formed by specific click chemistry reactions. In certain embodiments, these compounds, owing to the presence of the targeting moiety, can cross the blood-brain barrier or accumulate in the lysosome more effectively than the enzyme alone. The invention also features pharmaceutical compositions containing such compounds and methods for treating lysosomal storage disorders (e.g., mucopolysaccharidosis Type II) using such compounds.