AZN

Pyrimidine analog chemotherapy that inhibits thymidylate synthase, blocking DNA synthesis. Foundational in colorectal, breast, and head/neck cancers (FOLFOX, FOLFIRI regimens).

Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins.

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.

Oral second-generation Bruton's tyrosine kinase inhibitor (Calquence). Approved in chronic lymphocytic leukemia, mantle cell lymphoma, and small lymphocytic lymphoma.

The growth of many cancers of the breast is stimulated or maintained by estrogens. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol.

Anifrolumab-fnia is a human IgG1κ monoclonal antibody that binds to subunit 1 of the type I interferon receptor (IFNAR) with high specificity and affinity.

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

Benralizumab is a humanized afucosylated, monoclonal antibody (IgG1, kappa) that directly binds to the alpha subunit of the human interleukin-5 receptor (IL-5Rα) with a dissociation constant of 11 pM.

Anti-VEGF-A monoclonal antibody (Avastin) that inhibits tumor angiogenesis. Approved for colorectal, ovarian, breast, glioblastoma, and other solid tumors.

Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins.

Oral next-generation selective estrogen receptor degrader (AZD9833) in late-stage development for HR-positive HER2-negative breast cancer, including ESR1-mutant disease.

Oral 5-fluorouracil prodrug activated to 5-FU in tumor tissue. Used in colorectal, breast, and gastric cancers, often combined with oxaliplatin or platinum.

Capivasertib is an inhibitor of all 3 isoforms of serine/threonine kinase AKT (AKT1, AKT2 and AKT3) and inhibits phosphorylation of downstream AKT substrates.

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.

Carfilzomib is a tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds to the N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome.

Chimeric anti-EGFR monoclonal antibody (Erbitux) that blocks EGFR signaling and triggers ADCC. Approved in metastatic colorectal cancer (KRAS wild-type) and head and neck cancer.

Chlorambucil, an aromatic nitrogen mustard derivative, is an alkylating agent. Chlorambucil interferes with DNA replication and induces cellular apoptosis via the accumulation of cytosolic p53 and subsequent activation of Bax, an apoptosis promoter.

Platinum-based chemotherapy that forms DNA crosslinks. Foundational cytotoxic agent used across testicular, bladder, ovarian, head and neck, and lung cancers.

Alkylating chemotherapy that forms DNA crosslinks. Backbone in lymphoma (R-CHOP), breast cancer, and as conditioning regimen for stem cell transplant.

Sodium-glucose cotransporter 2 (SGLT2), expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen.

Anti-CD38 monoclonal antibody (Darzalex). Approved across multiple myeloma settings; subcutaneous formulation marketed as Darzalex Faspro.

Darolutamide is an androgen receptor (AR) inhibitor. Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR-mediated transcription. A major metabolite, ketodarolutamide, exhibited similar in vitro activity to darolutamide.

Datopotamab deruxtecan: anti-TROP2 antibody conjugated to a topoisomerase I inhibitor payload. Approved in HR-positive HER2-negative breast cancer; under investigation in NSCLC.

Anti-TROP2 antibody (Dato-DXd, Datroway) conjugated to a topoisomerase I inhibitor payload. Approved in HR-positive HER2-negative breast cancer; under investigation in NSCLC.

Datopotamab deruxtecan (Datroway): anti-TROP2 antibody conjugated to a topoisomerase I inhibitor payload. Approved in HR+/HER2- breast cancer; under investigation in NSCLC.

Synthetic corticosteroid widely used as anti-inflammatory and immunosuppressant. In oncology, used in multiple myeloma regimens and as supportive care for chemotherapy-induced nausea/edema.

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

Anthracycline chemotherapy that intercalates DNA and inhibits topoisomerase II. Backbone agent in breast cancer, lymphoma, leukemia, and sarcoma regimens.

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.

Enfortumab vedotin-ejfv is an ADC. The antibody is a human IgG1 kappa directed against Nectin-4, an adhesion protein located on the surface of cells. The small molecule, MMAE, is a microtubule-disrupting agent, attached to the antibody via a protease-cleavable linker.

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

Eplontersen is an antisense oligonucleotide-GalNAc conjugate that causes degradation of mutant and wild-type TTR mRNA through binding to the TTR mRNA, which results in a reduction of serum TTR protein and TTR protein deposits in tissues.

Eribulin inhibits the growth phase of microtubules without affecting the shortening phase and sequesters tubulin into nonproductive aggregates.

Eribulin inhibits the growth phase of microtubules without affecting the shortening phase and sequesters tubulin into nonproductive aggregates.

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

Breast cancer cell growth may be estrogen-dependent. Aromatase is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women.

Injectable selective estrogen receptor degrader (Faslodex) that binds and degrades ERα. Used in HR-positive metastatic breast cancer.

Pyrimidine nucleoside analog chemotherapy that incorporates into DNA and inhibits ribonucleotide reductase. First-line in pancreatic cancer; used in lung, breast, and bladder cancers.

Anti-CTLA-4 monoclonal antibody (Yervoy) that releases T-cell inhibition early in immune activation. Approved in melanoma, RCC, MSI-H colorectal, and other cancers, often combined with nivolumab.

Topoisomerase I inhibitor chemotherapy that prevents DNA religation. Used in colorectal cancer (FOLFIRI) and other GI cancers.

Oral non-steroidal aromatase inhibitor (Femara) that blocks estrogen synthesis. Standard endocrine therapy in HR-positive postmenopausal breast cancer.

Reduced folate used to rescue normal cells from methotrexate toxicity and to potentiate 5-FU activity (FOLFOX, FOLFIRI). Not a primary anticancer agent.

Mepolizumab is an IL-5 antagonist (IgG1 kappa). IL-5 is the major cytokine responsible for the growth and differentiation, recruitment, activation, and survival of eosinophils.

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.

Albumin-bound paclitaxel (Abraxane) with improved delivery and reduced solvent toxicity. Used in metastatic breast cancer, NSCLC, and pancreatic adenocarcinoma.

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

Glycoengineered Type II anti-CD20 monoclonal antibody (Gazyva) with enhanced ADCC. Approved in chronic lymphocytic leukemia and follicular lymphoma.

Oral PARP inhibitor (Lynparza) that exploits synthetic lethality in BRCA-mutant cancers. Approved in BRCA-mutant ovarian, breast, prostate, and pancreatic cancer.

Olaparib (Lynparza) 300mg dosing form. Oral PARP inhibitor approved in BRCA-mutant ovarian, breast, prostate, and pancreatic cancer.

Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) at approximately 9-fold lower concentrations than wild-type.

Third-generation platinum chemotherapy that forms DNA adducts. Backbone in colorectal cancer (FOLFOX) and other GI malignancies.

Taxane chemotherapy that binds β-tubulin and prevents microtubule depolymerization, causing mitotic arrest. Used in breast, ovarian, lung, and other cancers.

First-in-class oral CDK4/6 inhibitor (Ibrance) approved in HR-positive HER2-negative metastatic breast cancer in combination with endocrine therapy.

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.

Multi-targeted antifolate chemotherapy used in non-squamous NSCLC and mesothelioma, typically combined with platinum agents.

Pertuzumab targets the extracellular dimerization domain (Subdomain II) of the human epidermal growth factor receptor 2 protein (HER2) and, thereby, blocks ligand-dependent heterodimerization of HER2 with other HER family members, including EGFR, HER3, and HER4.

Pomalidomide is an analogue of thalidomide with immunomodulatory, antiangiogenic, and antineoplastic properties. Cellular activities of pomalidomide are mediated through its target cereblon, a component of a cullin ring E3 ubiquitin ligase enzyme complex.

Oral selective CDK4/6 inhibitor (Kisqali) that blocks cell-cycle progression. Approved in HR-positive HER2-negative metastatic and adjuvant breast cancer.

Bispecific antibody (AstraZeneca) targeting both PD-1 and TIGIT checkpoints. Phase 3 in NSCLC, biliary tract cancer, and other solid tumors.

Chimeric anti-CD20 monoclonal antibody (Rituxan) that depletes B cells via ADCC, CDC, and apoptosis. Foundational in B-cell lymphomas, CLL, rheumatoid arthritis, and ANCA vasculitis.

Oral selective c-MET kinase inhibitor approved in China for MET exon 14-mutant NSCLC. Under investigation in MET-driven NSCLC, papillary RCC, and gastric cancer.

Selumetinib is an inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2). MEK1/2 proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway.

Oral multi-kinase inhibitor (Sutent) targeting VEGFR, PDGFR, and c-KIT. Approved in renal cell carcinoma, GIST, and pancreatic neuroendocrine tumors.

Tamoxifen is an estrogen agonist/antagonist. Tamoxifen competes with estrogen for binding to the estrogen receptor, which can result in a decrease in estrogen receptor signaling-dependent growth in breast tissue.

Tezepelumab-ekko is a thymic stromal lymphopoietin (TSLP) blocker, human monoclonal antibody IgG2λ that binds to human TSLP with a dissociation constant of 15.8 pM and blocks its interaction with the heterodimeric TSLP receptor.

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

Anti-HER2 monoclonal antibody (Herceptin) that binds the extracellular domain of HER2, blocking signaling and triggering ADCC. Standard of care in HER2-positive breast and gastric cancers.

Anti-HER2 antibody (trastuzumab) conjugated to a topoisomerase I inhibitor payload (deruxtecan). Approved in HER2-positive and HER2-low breast cancer, gastric cancer, and NSCLC. Also marketed as T-DXd, Enhertu.

Anti-CTLA-4 monoclonal antibody (Imjudo) that releases T-cell inhibition. Approved in combination with durvalumab in unresectable hepatocellular carcinoma and metastatic NSCLC.

Oral selective BCL-2 inhibitor (Venclexta) that restores apoptosis in cancer cells. Approved for chronic lymphocytic leukemia, acute myeloid leukemia, and small lymphocytic lymphoma.

Vinorelbine is a vinca alkaloid that interferes with microtubule assembly. The antitumor activity of vinorelbine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin.

Bispecific antibody (AstraZeneca) targeting both PD-1 and CTLA-4 checkpoints in a single molecule. Phase 3 in cervical cancer and other solid tumors.

Zolbetuximab-clzb is a claudin 18.2 (CLDN18.2)-directed cytolytic antibody that depletes CLDN18.2-positive cells via antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC).

5-fluorouracil. Pyrimidine analog chemotherapy that inhibits thymidylate synthase. Backbone in colorectal cancer regimens (FOLFOX, FOLFIRI).

Alectinib is a tyrosine kinase inhibitor that targets ALK and RET.

Amivantamab-vmjw is a bispecific antibody that binds to the extracellular domains of EGFR and MET.

Apalutamide is an Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription.

Oral selective MAT2A inhibitor (AstraZeneca) targeting MTAP-deleted cancers via synthetic lethality. Phase 1/2 in MTAP-deleted solid tumors.

Saruparib: oral next-generation selective PARP1 inhibitor (AstraZeneca) designed to spare PARP2 to reduce hematologic toxicity. Phase 3 in BRCA-mutant breast and prostate cancer.

Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP.

The epidermal growth factor receptor (EGFR) is expressed on the cell surface of both normal and cancer cells and plays a role in the processes of cell growth and proliferation.

Lenvatinib is a kinase inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4).

Necitumumab is a recombinant human lgG1 monoclonal antibody that binds to the human epidermal growth factor receptor (EGFR) and blocks the binding of EGFR to its ligands.

Posaconazole is an azole antifungal agent [ see Clinical Pharmacology (12.4) ].

Ramucirumab is a VEGFR2 antagonist that specifically binds VEGFR2 and blocks binding of VEGFR ligands, VEGF-A, VEGF-C, and VEGF-D.

Rosuvastatin is an inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3‑hydroxy‑3‑methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol.

Selpercatinib is a kinase inhibitor. Selpercatinib inhibited wild-type RET and multiple mutated RET isoforms as well as VEGFR1 and VEGFR3 with IC 50 values ranging from 0.92 nM to 67.8 nM.

Trastuzumab deruxtecan (Enhertu): anti-HER2 antibody conjugated to a topoisomerase I inhibitor payload. Approved in HER2-positive and HER2-low breast cancer, gastric cancer, and NSCLC.

Oral selective HER2 tyrosine kinase inhibitor (Tukysa) that crosses the blood-brain barrier. Used in HER2-positive metastatic breast cancer including patients with brain metastases.

Vinca alkaloid chemotherapy that inhibits microtubule polymerization, arresting mitosis. Used in lymphomas (R-CHOP), leukemias, and pediatric cancers.