# US 11,077,201 B2 · Immunoconjugates with an intracellularly-cleavable linkage

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- Number: US 11,077,201 B2
- Document ID: US11077201B2
- Status: Granted
- Kind: B2
- Application number: 16/733,816
- Filed: 2020-01-03
- Published: 2020-04-23
- Granted: 2021-08-03
- Earliest claimed: 2002-12-13
- Assignees: Immunomedics, Inc.
- Applicants: Immunomedics, Inc.
- Inventors: Serengulam V. Govindan; Sung-Ju Moon; David M. Goldenberg
- Web page: https://patentgrep.com/patent/US11077201B2

## CPC

- C07K 16/1145: {Env proteins, e.g. gp41, gp110/120, gp160, V3, principal neutralising domain [PND] or CD4-binding site}
- A61K 31/4745: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/68037: {the drug being a camptothecin [CPT] or derivatives}
- A61K 47/6841: {the antibody targeting a RNA virus}
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- A61K 47/6851: {the antibody targeting a determinant of a tumour cell}
- A61K 47/6853: {Carcino-embryonic antigens}
- A61K 47/6855: {the tumour determinant being from breast cancer cell}
- A61K 47/6857: {the tumour determinant being from lung cancer cell}
- A61K 47/6859: {the tumour determinant being from liver or pancreas cancer cell}
- A61K 47/6861: {the tumour determinant being from kidney or bladder cancer cell}
- A61K 47/6889: {Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment}
- A61N 5/10: X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy (A61N5/01 takes precedence)
- A61P 17/00: Drugs for dermatological disorders
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/12: Antivirals
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- C07D 491/22: in which the condensed system contains four or more hetero rings
- C07K 16/18: against material from animals or humans
- C07K 16/2803: {against the immunoglobulin superfamily}
- C07K 16/2833: {against MHC-molecules, e.g. HLA-molecules}
- C07K 16/2863: {against receptors for growth factors, growth regulators}
- C07K 16/2887: {against CD20}
- C07K 16/30: from tumour cells
- C07K 16/303: {Liver or Pancreas}
- C07K 16/3046: {Stomach, Intestines}
- C07K 16/3076: {against structure-related tumour-associated moieties}
- C07K 16/3092: {against tumour-associated mucins}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/31: multispecific
- C07K 2317/40: characterized by post-translational modification
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/53: Hinge
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61N: ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY (measurement of bioelectric currents A61B; surgical instruments, devices or methods for transferring non-mechanical forms of energy to or from the body A61B18/00; anaesthetic apparatus in general A61M; incandescent lamps H01K; infrared radiators for heating H05B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention relates to therapeutic conjugates with improved ability to target various diseased cells containing a targeting moiety (such as an antibody or antibody fragment), a linker and a therapeutic moiety, and further relates to processes for making and using the conjugates.

## Claims

### Claim 1

An antibody-drug conjugate (ADC) having a structural formula MAb-CL2A-SN-38, with a structure represented by:
wherein the MAb is hRS7.

### Claim 2 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the MAb is a monoclonal antibody or an antigen binding antibody fragment.

### Claim 3 (depends on 2)

The antibody-drug conjugate of claim 2, wherein said fragment is selected from the group consisting of Fab, Fab′, F(ab)2, F(ab′)2, and scFv.

### Claim 4 (depends on 2)

The antibody-drug conjugate of claim 2, wherein the MAb has constant domains and a hinge domain of a human IgG1 antibody.

### Claim 5 (depends on 1)

The antibody-drug conjugate of claim 1, wherein said MAb is attached to between 1 and 12 copies of the CL2A-SN38.

### Claim 6 (depends on 1)

The antibody-drug conjugate of claim 1, wherein said MAb is attached to between 6 and 8 copies of CL2A-SN38.

### Claim 7 (depends on 1)

The antibody-drug conjugate of claim 1, wherein said MAb is attached to between 1 and 5 copies of CL2A-SN38.