PFE

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

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

CIBINQO is a Janus kinase (JAK) inhibitor. Abrocitinib reversibly inhibits JAK1 by blocking the adenosine triphosphate (ATP) binding site.

PD-L1 may be expressed on tumor cells and tumor-infiltrating immune cells and can contribute to the inhibition of the anti-tumor immune response in the tumor microenvironment.

Axitinib has been shown to inhibit receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3 at therapeutic plasma concentrations.

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

Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway.

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.

CD30 is a member of the tumor necrosis factor receptor family and is expressed on the surface of sALCL cells and on Hodgkin Reed-Sternberg (HRS) cells in cHL. CD30 is variably expressed in other T-cell lymphomas.

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

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.

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

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

Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON).

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

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.

Anti-HER2 antibody conjugated to monomethyl auristatin E (MMAE), a microtubule disruptor. Approved in China for HER2-overexpressing urothelial and gastric cancers.

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

Elotuzumab is a humanized IgG1 monoclonal antibody that specifically targets the SLAMF7 (Signaling Lymphocytic Activation Molecule Family member 7) protein. SLAMF7 is expressed on myeloma cells independent of cytogenetic abnormalities.

Elranatamab-bcmm is a bispecific B-cell maturation antigen (BCMA)-directed T-cell engaging antibody that binds BCMA on plasma cells, plasmablasts, and multiple myeloma cells and CD3 on T-cells leading to cytolysis of the BCMA-expressing cells.

Encorafenib is a kinase inhibitor that targets BRAF V600E, as well as wild-type BRAF and CRAF in in vitro cell-free assays with IC 50 values of 0.35, 0.47, and 0.3 nM, respectively.

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

Everolimus is an inhibitor of mammalian target of rapamycin (mTOR), a serine-threonine kinase, downstream of the PI3K/AKT pathway. The mTOR pathway is dysregulated in several human cancers and in tuberous sclerosis complex (TSC).

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.

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

Oral immunomodulatory drug (Revlimid) that recruits IKZF1/IKZF3 to cereblon for degradation. Standard in multiple myeloma, MDS, and follicular lymphoma.

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.

High-Dose Methotrexate Therapy Levoleucovorin is the pharmacologically active isomer of 5-formyl tetrahydrofolic acid.

Lorlatinib is a kinase inhibitor with in vitro activity against ALK and ROS1 as well as TYK1, FER, FPS, TRKA, TRKB, TRKC, FAK, FAK2, and ACK.

Marstacimab‑hncq is a human monoclonal IgG1 antibody directed against the Kunitz domain 2 (K2) of TFPI to neutralize TFPI activity and enhance coagulation.

Nirmatrelvir is a severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) antiviral drug [see Microbiology (12.4) ]. Ritonavir is an HIV-1 protease inhibitor but is not active against SARS-CoV-2 M pro .

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

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.

Remdesivir is an antiviral drug with activity against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) [see Microbiology (12.4) ].

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

Rimegepant is a calcitonin gene-related peptide receptor antagonist.

LITFULO is a kinase inhibitor. Ritlecitinib irreversibly inhibits Janus kinase 3 (JAK3) and the tyrosine kinase expressed in hepatocellular carcinoma (TEC) kinase family by blocking the adenosine triphosphate (ATP) binding site.

Lopinavir and ritonavir tablets are a fixed-dose combination of HIV-1 antiviral drugs lopinavir [see Microbiology ( 12.4 )] and ritonavir.

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.

Talazoparib is an inhibitor of PARP enzymes, including PARP1 and PARP2, which play a role in DNA repair.

Tofacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function.

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.

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.

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

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

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

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.

Etrasimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1, 4, and 5 (S1P 1,4,5 ). Etrasimod has minimal activity on S1P 3 (25-fold lower than C max at the recommended dose) and no activity on S1P 2 .

Glofitamab-gxbm is a bispecific antibody that binds to CD20 expressed on the surface of B cells, and to CD3 receptor expressed on the surface of T cells. Glofitamab-gxbm causes T-cell activation and proliferation, secretion of cytokines, and the lysis of CD20-expressing B cells.

Inotuzumab ozogamicin is a CD22-directed antibody drug conjugate (ADC). Inotuzumab recognizes human CD22. The small molecule, N-acetyl-gamma-calicheamicin, is a cytotoxic agent that is covalently attached to the antibody via a linker.

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.

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

Oral DNA-methylating chemotherapy that crosses the blood-brain barrier. Standard of care in glioblastoma multiforme; also used in melanoma.

Tisotumab vedotin-tftv is a tissue factor (TF)-directed antibody drug conjugate (ADC). The antibody is a human IgG1 directed against cell surface TF. TF is the primary initiator of the extrinsic blood coagulation cascade.

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