American Chemical Society Spring Meeting Highlights: These Molecules Bring New Breakthroughs to Old Targets

A number of biopharmaceutical and technology companies announced the chemical structures of their therapeutic candidates for the first time at the American Chemical Society (ACS) Spring 2022 meeting "First-time Disclosures" symposium

Drug Candidate: LY3372689

R&D organization: Eli Lilly

Target: O-GlcNAzyme

Disease area: Alzheimer's disease

Image source: Reference [1]

Alzheimer's disease affects the lives of nearly 40 million people worldwide

Eli Lilly researchers found that blocking OGA in a mouse model slowed tau protein aggregation by 50 percent

Drug Candidate: AZD9574

R&D organization: AstraZeneca

Target: PARP1

Disease Area: Cancer

Image source: Reference [1]

The PARP family of proteases plays an important role in the DNA damage response, and existing PARP1 and PARP2 inhibitors have been approved for the treatment of various cancer types harboring DNA damage response defects

However, this compound cannot effectively enter the central nervous system.

Drug Candidate: PF-07038124

R&D organization: Pfizer

Target: Phosphodiesterase 4

Disease Area: Inflammatory Skin Diseases

Image source: Reference [1]

Phosphodiesterase 4 (PDE4) inhibitors are one of the important therapeutic options for the treatment of atopic dermatitis, psoriasis and other inflammatory skin diseases

▲ The results of the Phase 2a trial of PF-07038124 in the treatment of patients with atopic dermatitis (Image source: Pfizer official website)

With anti-IL-4 and anti-IL-13 antibodies emerging as powerful options for the treatment of inflammatory skin diseases, this topical PDE4 inhibitor offers new opportunities for combination with biologics

Drug Candidate: BLU-945

Research and development organization: Blueprint Medicines

Target: Epidermal Growth Factor Receptor (EGFR)

Disease area: Drug-resistant non-small cell lung cancer

Image source: Reference [1]

Targeting EGFR is one of the main ways to treat non-small cell lung cancer

BLU-945 is an oral fourth-generation EGFR inhibitor that inhibits the activity of EGFR with double or triple mutations

▲BLU-945 dose-dependently reduces circulating tumor DNA (Image source: Blueprint Medicines official website)

Drug Candidate: KVD900

Research and Development Organization: KalVista Pharmaceuticals

Target: Plasma kallikrein

Disease Area: Hereditary Angioedema

Image source: Reference [1]

Hereditary angioedema (HAE) is a rare and potentially fatal genetic disorder characterized by rapid and painful onset of inflammation of the hands, feet, extremities, face, abdomen, larynx, and airways

KVD900 is an oral plasma kallikrein inhibitor targeted as acute therapy for the treatment of angioedema episodes in patients with HAE

Drug Candidate: AMG 650

R&D organization: Amgen

Target: Kinesin family member 18A (KIF18A)

Disease Area: Advanced Solid Tumors

Image source: Reference [1]

Kinesins are a group of molecular motor proteins that help separate chromosomes

AMG 650 is a potential "first-in-class" oral KIF18A inhibitor currently being evaluated in a Phase 1 clinical trial for the treatment of solid tumors

References:

[1] In Context: First-Time Disclosures of ACS Spring 2022.