A61K47/6863

Bifunctional cytotoxic agents containing the CTI pharmacophore

The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula:
F.sup.1-L.sup.1-T-L.sup.2-F.sup.2
where F.sup.1, L.sup.1, T, L.sup.2 and F.sup.2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.

ANTIBODIES AND ENONOMERS
20220175945 · 2022-06-09 ·

The subject invention provides a composition comprising an enomomer which comprises a) a carrier molecule, and b) at least one aptamer, wherein the carrier molecule is an antibody, an antigen-binding moiety, a serum protein, an intracellular protein, a messenger RNA (mRNA) or human serum albumin.

DRUG CONJUGATES COMPRISING ANTIBODIES AGAINST CLAUDIN 18.2

The present invention provides anti-CLDN18.2 antibody-drug conjugates which are effective for treating and/or preventing cancer diseases associated with cells expressing CLDN18.2, including gastric cancer, esophageal cancer, pancreatic cancer, lung cancer, ovarian cancer, colon cancer, hepatic cancer, head-neck cancer, and cancer of the gallbladder and metastases thereof.

AZETIDOBENZODIAZEPINE DIMERS AND CONJUGATES COMPRISING THEM FOR USE IN THE TREATMENT OF CANCER
20220160881 · 2022-05-26 ·

A compound of formula IV: as well as drug-linkers and conjugates comprising this compound, and the use of the conjugates in treating cancer.

##STR00001##

Monoclonal antibodies against Claudin-18 for treatment of cancer

The present invention provides antibodies useful as therapeutics for treating and/or preventing diseases associated with cells expressing CLD18, including tumor-related diseases such as gastric cancer, esophageal cancer, pancreatic cancer, lung cancer, ovarian cancer, colon cancer, hepatic cancer, head-neck cancer, and cancer of the gallbladder.

Immunoconjugates Targeting CEA

The invention provides an immunoconjugate of formula (I) or (II) Antibody-adjuvant immunoconjugates of the invention, comprising an antibody construct that has an antigen binding domain that binds carcinoembryonic antigen (“CEA”) linked to one or more adjuvants, demonstrate superior pharmacological properties over conventional antibody conjugates. The invention further provides compositions comprising and methods of treating cancer with the immunoconjugate.

ANTI-FGFR2 ANTIBODIES AND METHODS OF USE THEREOF
20220162323 · 2022-05-26 ·

Provided herein are monoclonal antibodies, and antigen-binding fragments thereof, that bind fibroblast growth factor receptor 2 (FGFR2), and methods of use thereof and methods of use thereof. Also included are antibody-drug conjugates (ADCs) comprising the anti-FGFR2 antibodies or antigen-binding fragments thereof linked to a cytotoxic agent, radionuclide, or other moiety, as well as methods of treatment using the same.

Conjugates of cell binding molecules with cytotoxic agents

A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a Formula (I), wherein T, L, m, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, and R.sup.13 are defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.

Saponin Conjugates

The current invention relates to an effector moiety capable of inducing an intracellular effect when present inside a mammalian cell, the effector moiety comprising a payload conjugated with at least one saponin. The invention also relates to an antibody-drug conjugate comprising the effector moiety according to the invention, or a ligand-drug conjugate comprising the effector moiety of the invention, the effector moiety comprising covalently coupled saponin. The invention also relates to a therapeutic combination comprising: (a) the effector moiety of the invention, comprising at least one saponin, and optionally a pharmaceutically acceptable excipient; and (b) an antibody-drug conjugate or a ligand-drug conjugate, and optionally a pharmaceutically acceptable excipient. Further, the invention relates to a pharmaceutical composition comprising the effector moiety of the invention or the antibody-drug conjugate of the invention or the ligand-drug conjugate of the invention, comprising at least one saponin covalently linked to the effector molecule, and optionally a pharmaceutically acceptable excipient. The invention also relates to the effector moiety of the invention or the antibody-drug conjugate of the invention or the therapeutic combination of the invention or the ligand-drug conjugate of the invention or the pharmaceutical composition of the invention, for use as a medicament. Finally, the invention also relates to the effector moiety of the invention or the antibody-drug conjugate of the invention or the therapeutic combination of the invention or the ligand-drug conjugate of the invention or the pharmaceutical composition of the invention, for use in the treatment or prevention of a cancer or an autoimmune disease.

ANTI-ERBB2 ANTIBODY-DRUG CONJUGATE AND COMPOSITION THEREOF, PREPARATION METHOD THEREFOR, AND USE THEREOF

Provided is a method for the prophylaxis or treatment of cancer, comprising administering to a patient in need thereof an antibody-drug conjugate represented by Formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof, or a solvate of the foregoing,

##STR00001##

wherein A, X, Y, L, D and a are as defined herein.