A61K47/6855

ANTIBODY DRUG CONJUGATES COMPRISING STING AGONISTS

The present disclosure provides scaffolds and antibody-drug conjugates (ADCs) comprising a stimulator of interferon genes (STING). The present disclosure also provides uses of the ADCs in treatment, e.g., treatment of cancer.

DIELS-ALDER CONJUGATION METHODS
20220378918 · 2022-12-01 · ·

Described herein are protein-payload conjugates and compositions thereof that are useful, for example, for target-specific delivery of therapeutic and/or imaging agent moieties. In certain embodiments, provided are specific and efficient methods for producing protein-payload constructs (e.g., antibody-drug conjugates) utilizing a combination of transglutaminase and Diels-Alder techniques. Antibody-drug conjugates and compositions which comprise glutaminyl-modified antibodies, Diels-Alder adducts, and reactive payloads and are provided.

BENZOSELENOPHENE-BASED COMPOUND, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND ANTIBODY-DRUG CONJUGATE
20220380360 · 2022-12-01 ·

The present disclosure relates to a benzoselenophene-based compound, a method of preparing the benzoselenophene-based compound, and a pharmaceutical composition and antibody-drug conjugate including the benzoselenophene-based compound.

TRANSGLUTAMINASE-MEDIATED CONJUGATION

The present disclosure provides for antibody-oligonucleotide conjugates, methods of preparation thereof, and methods of use thereof. Also provided are related compounds, compositions and kits.

ANTI-HER2 ANTIBODY-DRUG CONJUGATES AND USES THEREOF
20220378929 · 2022-12-01 ·

Disclosed are new anti-HER2 ADCs conjugated to camptothecin derivatives as toxins for therapeutic use. The antitumor effects of the ADCs of Formula (PL-A) (e.g., compounds MB-2a and MB-3a (trastuzumab meditecan)) render these compounds useful for treating cell proliferative diseases such as cancers.

##STR00001##

ANTIBODY-IMMUNE AGONIST CONJUGATE AND APPLICATIONS THEREOF
20220378930 · 2022-12-01 ·

The present disclosure relates to a linking unit molecule for targeting molecule-drug conjugate, and the corresponding conjugate, the preparation and use thereof, and in particular relates to an antibody-immune agonist conjugate (AIAC) as a novel type of cancer therapy.

Modified microcystins and nodularins

A compound includes cytotoxic agents such as microcystin and nodularin. More specifically, a modified microcystin and/or nodularin compound contains one or more modified substrates, wherein one or more modified substrates include an anchor group directly accessible or transformable for use in conjugation chemistry (incl. click chemistry), for the attachment of a targeting moiety. This compound is useful for cancer treatment.

Cytotoxic and anti-mitotic compounds, and methods of using the same

Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

Antibody glycoconjugates and methods of production and use

The present invention relates to compounds, compositions, and methods are provided for covalently linking a cargo molecule, such as a therapeutic or a diagnostic agent, to a glycan in the Fab region of an antibody. Also provided are methods of modeling and producing antibodies having de novo Fab glycosylation sites. Also provided are antibody carrier conjugates, methods of using the conjugates.

Diagnosis and treatment of cancer

The present invention relates to compositions and methods for cancer therapy, including but not limited to, therapies that utilize cancer biomarkers. In particular, the present invention relates to compositions and methods for the prediction of a subject's response to cancer therapies.