Cancer Immunotherapy: mAbs and Checkpoint Inhibitors

Photodynamic Therapy

• Methoxsalen (Uvadex) inhibits DNA synthesis and damages DNA.

Retinoids

• Tretinoin (ATRA) activates PML-RAR, inhibiting differentiation and increasing normal white blood cells (WBCs).
• ATRA can cause RA-APL syndrome, characterized by leukocytosis (increased WBCs) and immune system effects.
• Bexarotene activates RXR.

PD-1/T-cell Checkpoint Inhibitors

• Pembrolizumab or Nivolumab block immune cell (T-cell) inhibition via PD-1, enhancing immune response and treating multiple cancers.

Anti-CD19 and CD20 mAbs

• Anti-CD19 mAbs (-tamab, -tuximab, -tumomab, -tuzumab) target CD19.
  • Tafasitamab and loncastuximab are examples of CD19-targeting mAbs.
• Anti-CD20 mAbs target CD20.
  • Rituximab, ofatumumab, obintuzumab, and ibritumomab are examples of CD20-targeting mAbs, some targeting Type I CD20 and others Type II CD20.

Anti-CD22 mAbs

• Inotuzumab ozogamicin targets CD22.

Anti-CD30 or CD79b mAbs

• Brentuximab vedotin inhibits tubulin polymerization and can induce peripheral neuropathy.

Anti-CD38 or SLAMF mAbs

• -tuximab and -tumumab target CD38 or SLAMF.

BITE Antibodies

• These antibodies, like -tumomab, -tuzumab, and -tamab, target CD3 and CD19 or CD3 and BCMA.
• Can cause cytokine release syndrome (CRS) and neurotoxicity.

STI's that block JAK

• Fedratinib, pacritinib, and ruxolitinib block JAK.

STI's that block BTK

• Ibrutinib, acalabrutinib, and zanubrutinib and pirtobrutinib block BTK.

Block Ph and c-KIT Inhibitors

• Some -a/-o/-utinib inhibitors block Ph and c-KIT (except fedratinib).
• Asciminib is specific for Ph.

Block FLT3 Inhibitors

• Midostaurin, gilteritinib, and quizartinib (Vanflyta) block FLT3.

SMO Blockers

• Glasdegib blocks SMO.

Block PKB at PI3K

• Idelalisib and duvelisib block PKB at PI3K.

Black Protein Synthesis Inhibitors

• Omacetaxine mepesuccinate (Synribo) inhibits protein synthesis by binding to ribosomes.

Proteasome Inhibitors

• Bortezomib, carfilzomib, and ixazomib inhibit proteasome activity.

Block DNA Condensation via HDAC

• Romidepsin, vorinostat, belinostat, and panobinostat block DNA condensation via HDAC.

Block DNA Condensation via HMT

• Tazemetostat blocks DNA condensation via HMT.

Block BCL-2

• Venetoclax blocks BCL-2.

Mutant IDH Blockers

• Ivosidenib, enasidenib, and olutasidenib are Mutant IDH Blockers, influencing differentiation.

Inhibit Nuclear Transport (Exportin 1)

• Selinexor inhibits nuclear transport (Exportin 1).

Block Menin/Aberrant Transcription

• Revumenib blocks menin and aberrant transcription.

Inhibit Telomerase

• Imetelstat (Rytelo) inhibits telomerase.

CAR-T Therapy

• Lisocabtagene maraleucel targets CD19 (except idecabtagene vicleucel and ciltacabtagene autoleucel).

Miscellaneous Agents

• Hydroxyurea inhibits ribonucleotide reductase, and DNA synthesis.
• Asparaginase depletes asparagine from the plasma.
• Arsenic trioxide degrades PML-RAR-α, causing differentiation.

Thalidomide

• Increases IL-2 and interferon gamma, activating NK cells and inhibiting myeloid cell growth.

mAbs/STIs Summary of Protein Drugs with Immune Cell Targets

• Various drugs targeting specific markers on immune cells (e.g., CD19, CD20, CD38) are listed by their targets and the types of cancers they treat.

mAbs/STIs Summary of Protein Drugs with Immune Cell Targets (additional information)

• Drugs targeting specific immune cells and cancers are presented with their targets and affected types of cancer.

Summary of Miscellaneous STIs

• Ivosidenib, enasidenib, olutasidenib, vorasidenib, and other drugs target different pathways and are used to treat various cancers, like AML, astrocytomas, and CLL.

Summary of Cellular Therapies

• Different cellular therapies and their corresponding targets and cancers are listed.

Miscellaneous Antineoplastic Agents

• Various antineoplastic agents with their mechanisms of action and uses are listed, including drugs for anemia, neutropenia, and thrombocytopenia.

Summary of Anti-Emetics

• Different anti-emetic medications, their targets, and when they are helpful for treating nausea and vomiting are discussed.

Explore cancer immunotherapy, including photodynamic therapy with methoxsalen, retinoids like tretinoin and bexarotene, and PD-1/T-cell checkpoint inhibitors. Learn about anti-CD19, CD20, CD22, CD30, and CD79b mAbs and their mechanisms in enhancing immune response and treating cancers.