AMGN

Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 α-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis.

Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 α-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis.

Apremilast is an oral small molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels.

Avacopan is a complement 5a receptor (C5aR) antagonist that inhibits the interaction between C5aR and the anaphylatoxin C5a. Avacopan blocks C5a-mediated neutrophil activation and migration.

Bevacizumab products bind VEGF and prevent the interaction of VEGF to its receptors (Flt-1 and KDR) on the surface of endothelial cells.

Blinatumomab is a bispecific CD19-directed CD3 T-cell engager that binds to CD19 expressed on the surface of cells of B-lineage origin and CD3 expressed on the surface of T-cells.

Cabazitaxel is a microtubule inhibitor. Cabazitaxel binds to tubulin and promotes its assembly into microtubules while simultaneously inhibiting disassembly.

Platinum-based chemotherapy that forms DNA crosslinks, inducing apoptosis in cancer cells. Standard of care across many solid tumors including NSCLC, ovarian, breast, bladder, and biliary cancers.

Generic 'chemotherapy' label without a specific agent identified. Indicates a cytotoxic regimen used as comparator or backbone.

Taxane chemotherapy that stabilizes microtubules and arrests mitosis. Used in breast, prostate, NSCLC, head and neck, and gastric cancers.

Anti-PD-L1 monoclonal antibody (Imfinzi) that blocks PD-L1, restoring T-cell anti-tumor activity. Approved in NSCLC, SCLC, biliary tract cancer, and hepatocellular carcinoma.

Oral second-generation androgen receptor antagonist (Xtandi) that blocks AR signaling. Approved in metastatic and non-metastatic castration-resistant prostate cancer.

Etelcalcetide is a calcimimetic agent that allosterically modulates the calcium-sensing receptor (CaSR). Etelcalcetide binds to the CaSR and enhances activation of the receptor by extracellular calcium.

Epipodophyllotoxin chemotherapy that inhibits topoisomerase II. Used in small cell lung cancer, testicular cancer, and lymphomas.

The mechanism by which inebilizumab-cdon exerts its therapeutic effects in NMOSD, IgG4-RD, and gMG is presumed to involve binding to CD19, a cell surface antigen presents on pre-B and mature B lymphocytes.

Lurbinectedin is an alkylating drug that binds guanine residues in the minor groove of DNA, forming adducts and resulting in a bending of the DNA helix towards the major groove.

MariTide (AMG 133, Amgen): GIP receptor antagonist–GLP-1 agonist peptide-antibody conjugate. Phase 3 in obesity and type 2 diabetes; Phase 2 in heart failure with preserved ejection fraction.

Methotrexate inhibits dihydrofolic acid reductase. Dihydrofolates must be reduced to tetrahydrofolates by this enzyme before they can be utilized as carriers of one-carbon groups in the synthesis of purine nucleotides and thymidylate.

Anti-PD-1 monoclonal antibody (Opdivo) that blocks the PD-1 checkpoint. Approved across melanoma, NSCLC, RCC, head and neck, hepatocellular, and other cancers.

The EGFR is a transmembrane glycoprotein that is a member of a subfamily of type I receptor tyrosine kinases, including EGFR, HER2, HER3, and HER4. EGFR is constitutively expressed in normal epithelial tissues, including the skin and hair follicle.

KRYSTEXXA is a uric acid specific enzyme which is a recombinant uricase and achieves its therapeutic effect by catalyzing the oxidation of uric acid to allantoin, thereby lowering serum uric acid.

Anti-PD-1 monoclonal antibody (Keytruda) that blocks the PD-1 checkpoint, restoring anti-tumor immune response. FDA-approved across many cancers including NSCLC, melanoma, and gastroesophageal cancer.

Nplate increases platelet production through binding and activation of the TPO receptor, a mechanism analogous to endogenous TPO.

EVENITY inhibits the action of sclerostin, a regulatory factor in bone metabolism. EVENITY increases bone formation and, to a lesser extent, decreases bone resorption.

Oral covalent KRAS G12C inhibitor (Lumakras) approved in KRAS G12C-mutant NSCLC and colorectal cancer. First-in-class targeted therapy for previously undruggable KRAS.

Bispecific T-cell engager (Imdelltra) targeting DLL3 on small cell lung cancer cells and CD3 on T cells. Approved in extensive-stage SCLC after platinum chemotherapy progression.

Teprotumumab-trbw's mechanism of action in patients with Thyroid Eye Disease has not been fully characterized. Teprotumumab-trbw binds to IGF-1R and blocks its activation and signaling.

Topoisomerase I inhibitor chemotherapy used in small cell lung cancer, ovarian cancer, and cervical cancer.