Medical Pharmacology: Immunopharmacology (Immunosuppressants/Immunomodulators) Practice Questions

Rilonacept: Mechanism of Action

"Rilonacept Ultrastructure with 3 main components: the ligand-binding-domain of the human IL-1 receptor, IL-1 receptor accessory protein, and the Fc portion of the human IgG1. Rilonacept 'pocket' binds to the IL-1α and IL-1β acting as an IL-1 trap blocking the interaction with their specific receptor. Fc indicates fragment crystillizable region; IL-1RAcP; IL-1 Receptor accessory protein; IL-1RI; IL-1 receptor; IL, interleukin. Attribution: Presti S Elajami T Reyaldeen R Anthony C Imazio M Klein A Emerging Therapies for Recurrent Pericarditis: Interleukin-1 inhibitors J Am Heart Assoc 2021; 10: e021685. 1-12 (Figure 3) https://www.ahajournals.org/doi/full/10.1161/JAHA.121.021685 (second sourced from Klein, below) Klein et al: Rationale for and design of a pivotable phase 3 trial to assess efficacy and safety of rilonacept, and interleukin-1α and interleukin-1β trap, in patients with recurrent pericarditis. AM Heart J. 220;228: 81-90. https://www.sciencedirect.com/science/article/abs/pii/S0002870320302106

Rilonacept: Mechanism of Action

"Rilonacept Ultrastructure with 3 main components: the ligand-binding-domain of the human IL-1 receptor, IL-1 receptor accessory protein, and the Fc portion of the human IgG1.
Rilonacept 'pocket' binds to the IL-1α and IL-1β acting as an IL-1 trap blocking the interaction with their specific receptor.
Fc indicates fragment crystillizable region; IL-1RAcP; IL-1 Receptor accessory protein; IL-1RI; IL-1 receptor; IL, interleukin.
Attribution:
- Presti S Elajami T Reyaldeen R Anthony C Imazio M Klein A Emerging Therapies for Recurrent Pericarditis: Interleukin-1 inhibitors J Am Heart Assoc 2021; 10: e021685. 1-12 (Figure 3) https://www.ahajournals.org/doi/full/10.1161/JAHA.121.021685 (second sourced from Klein, below)
- Klein et al: Rationale for and design of a pivotable phase 3 trial to assess efficacy and safety of rilonacept, and interleukin-1α and interleukin-1β trap, in patients with recurrent pericarditis. AM Heart J. 220;228: 81-90. https://www.sciencedirect.com/science/article/abs/pii/S0002870320302106

Source Material:
- Rothlin C Gutkind J Chapter 39 Immunosuppressants, Immunomodulation and Tolerance In Goodman & Gilman's The Pharmacological Basis of Therapeutics (Brunton LL Knollman BC eds) McGraw Hill LLC (2023).
- Lake D & Briggs A Ch 55 Immunopharmacology in Katzung's Basic & Clinical Pharmacology (Vanderah TW, ed) 16e McGraw Hill 2023.
- Arcalyst RxList https://www.rxlist.com/arcalyst-drug.htm#description
  Attribution: Klein A Imazio et al. (12 authors) Phase 3 Trial of Interleukin-1 Trap Rilonacept in Recurrent Pericarditis N Engl J Med 2021 Jan 7; 384(1): 313-41 https://pubmed.ncbi.nlm.nih.gov/33200890/
- Presti S Elajami T Reyaldeen R Anthony C Imazio M Klein A Emerging Therapies for Recurrent Pericarditis: Interleukin-1 inhibitors J Am Heart Assoc 2021; 10: e021685. 1-12 https://www.ahajournals.org/doi/full/10.1161/JAHA.121.021685
- Gillespie J Mathews R McDermott M Rilonacept in the management of cryopyrin-associated periodic syndromes (CAPS). Journal of Inflammation Research 2010: 3 1-8 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3218731/
- Chrouos G Ch 39 Adrenocorticosteroids & Adrenocortical Antagonists in Katzung's Basic & Clinical Pharmacology (Vanderah TW, ed) 16e McGraw Hill 2023
- Brezinski E Klickstein L Armstrong A Ch 46 Pharmacology of Immunosuppression in Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. (Golan DE Armstrong EJ Armstrong AW, eds) 4e 2017
- Ritter JM Flower R Henderson G Loke YK MacEwan D Robinson E Fullerton J Ch 25 Anti-inflammatory and Immunosuppressant Drugs Rang & Dale's Pharmacology 10e Elsevier 2024.
- Burchum J Rosenthal L Lehne's Pharmacology for Nursing Care Ch 72 Immunosuppressants Elsevier 2022.
- Burchum J Rosenthal L Lehne's Pharmacology for Nursing Care Ch 75 Glucocorticoids in Nonendrocrine Disorders Elsevier 2022.
- Burchum J Rosenthal L Lehne's Pharmacology for Nursing Care Ch 76 Drug Therapy for Rheumatoid Arthritis Elsevier 2022.
- Bass A Rogatsky Ch 32 Immunomodulatory Drugs in Goldman-Cecil Medicine (Goldman L Schafer, eds) Elsevier 26e 2020
- Leiva M Takemoto Ch 238 Immunosuppressants in Lippincott Illustrated Reviews: Pharmacology 8e ((Walen et al, eds) Wolters Kluwer 2023.
- Hall J Hall M Ch 78 Adrenocortical Hormones Guyton and Hall Textbook of Medical Physiology 14e Elsevier 2021.
- Waller DG Sampson A Hitchings Ch 38 The Immune Response and Immunosuppressant Drugs Medical Pharmacology & Therapeutics 6e Elsevier 2022
- Waller DG Sampson A Hitchings Ch 30 Rheumotoid Arthritis, Other Inflammatory Arthrides and Osteoarthritis Medical Pharmacology & Therapeutics 6e Elsevier 2022