2. IMMUNOSUPPRESSANTS
Drugs that suppress the immune response.
Inhibition of organ transplantation rejection.
Treatment of autoimmune diseases.
Treatment of Covid -19.
4. Recent advances in
immunosuppressants-
In recent years, a large number of structurally diverse
immunosuppressants have been discovered.
Some of them are undergoing clinical trials and may
soon enter into routine clinical practice.
These compounds are either chemical entities obtained
or biomaterials such as monoclonal antibodies/gene
products/proteins.
5. DIMETHYL FUMARATE(Tecfidera)
Dimethyl fumarate is an orally administered fumarate
ester recently FDA approved for first-line monotherapy
of multiple sclerosis.
Activate The Nuclear Factor(erythroid Derived 2) like 2
Transcriptional Pathway Reduction Of Oxidative
Stress Protect Nerve Cells From Inflammation.
6. Dosing and uses
Dosage Forms & Strengths
capsule, delayed-release
• 120mg
• 240mg
Multiple Sclerosis
9. Dosing and uses
Dosage Forms & Strengths
solution for injection
• 20mg/mL (once daily dosing)
• 40mg/mL (3 times/week dosing)
Multiple Sclerosis-
Indicated for the treatment of relapsing forms of
multiple sclerosis.
10.
11. DARATUMUMAB(Darzalex)
Daratumumab is an immunoglobulin G1
kappa monoclonal antibody developed by
Janssen and Genmab.
It was first described in the literature in 2010
as a monoclonal antibody that targets CD38+
multiple myeloma cells; the first of its kind.
15. ELOTUZUMAB
Elotuzumab is a humanized IgG1 (Immunoglobulin
G) monoclonal antibody.
Elotuzumab targets SLAMF7, also known as
Signaling Lymphocytic Activation Molecule Family
member 7, a cell surface glycoprotein.
16.
17. DOSING AND USES
Dosage Forms & Strengths
injection, lyophilized powder for reconstitution
• 300mg/vial
• 400mg/vial
Multiple Myeloma
Combination with lenalidomide and dexamethasone.
18.
19. DINUTUXIMAB
Dinutuximab is an IgG1 monoclonal human/mouse
chimeric antibody against GD2.
By binding to GD2, dinutiximab induces antibody-
dependent cell-mediated cytotoxicity and complement-
dependent cytotoxicity of tumor cells thereby leading to
apoptosis and inhibiting proliferation of the tumour.
20. DOSING AND USES
Dosage Forms & Strengths
solution for injection
• 17.5mg/5mL (3.5mg/mL)
Neuroblastoma
• Indicated in combination with granulocyte-macrophage colony-
stimulating factor (GM-CSF), interleukin-2 (IL-2), and 13-cis-
retinoic acid (RA) for pediatric patients with high-risk
neuroblastoma.
21.
22. Canakinumab(ILARIS)
Human monoclonal antibody targeted at interleukin -1
beta.
In inflammatory diseases,involving cryopyrin associated periodic
syndromes,
IL-1 beta is excessively activated.
The protein cryopyrin controls activation of IL-1 beta.
Canakinumab binds to IL-1 beta and neutralises its
inflammatory activity.
23. Dosing and uses
Dosage Forms & Strengths
powder for injection
• 180mg/vial (150mg/mL after
reconstitution
24. USES-
Cryopyrin-Associated Periodic Syndrome
Indicated for treatment of cryopyrin-associated periodic syndrome (CAPS), including
familial cold autoinflammatory syndrome and Muckle-Wells syndrome in adults and
children.
Tumor Necrosis Factor Receptor-Associated Periodic Syndrome
Hyperimmunoglobulin D Syndrome/Mevalonate Kinase Deficiency
Familial Mediterranean Fever
Still Disease
Indicated for the treatment of active Still disease, including adult-onset Still disease
(AOSD)
25. Adverse effects:
The most common adverse reactions involved the central
nervous system (headache and vertigo), gastrointestinal
system (diarrhea and nausea), neuromuscular and
skeletal system (musculoskeletal pain), and respiratory
system (rhinitis, nasopharyngitis and bronchitis).
Influenza was also reported.
26. RILONACEPT (Arcalyst)
Dimeric fusion protein which is an interleukin 1 inhibitor.
First drug to treat recurrent pericarditis approved by FDA in march 2021.
27. Rilonacept (rilonacept) is an IL-1α
and IL-1β inhibitor.
Rilonacept works as a trap for IL-
1α and IL-1β, binding and
neutralizing them.
It prevents IL-1α and IL-1β from
interacting with IL1R1, resulting in
suppression of the latter’s activity.
28. Dosing and Uses
Dosage Forms & Strengths
injection, lyophilized powder for reconstitution
• 220mg/vial
Cryopyrin Associated Periodic Syndromes
Deficiency of Interleukin-1 Receptor Antagonist
Pericarditis
Indicated to treat recurrent pericarditis and to reduce risk for recurrence.
30. Tocilizumab(Actemra)
Humanized monoclonal antibody against IL-6
receptor.
June 24, 2021: Emergency use authorization
(EUA) issued by the FDA for treatment of
coronavirus disease 2019 (COVID-19) in
hospitalized adults and pediatric patients
(aged >2 years).
31. Dosing and uses
Dosage Forms & Strengths
injectable solution
• 20mg/mL (4-, 10-, and 20-mL single-dose vials)
32. Uses
Rheumatoid Arthritis
Giant Cell Arteritis
Systemic Sclerosis-Associated Interstitial Lung Disease
Cytokine Release Syndrome
COVID-19 (EUA)
June 24, 2021: Emergency use authorization (EUA) issued by the FDA
for treatment of coronavirus disease 2019 (COVID-19) in
hospitalized adults and pediatric patients (aged >2 years).
34. SILTUXIMAB(SYLVANT)
Siltuximab is a chimeric (human-mouse) monoclonal
immunoglobulin G1-kappa antibody produced in a Chinese hamster
ovary (CHO) cell line by recombinant DNA technology.
Siltuximab complexes with human IL-6 and prevents binding to
soluble and membrane-bound IL-6 receptors, thereby inhibiting the
proliferation of lymphocytes.
35. Dosing and Uses
Dosage Forms & Strengths
lyophilized powder for reconstitution
• 100mg/vial
• 400mg/vial
Castleman Disease
Indicated for multicentric Castleman disease in patients who
are negative for HIV and human herpesvirus-8.
36. Adverse effects
Pruritis, increased weight, rash, hyperuricemia
and upper respiratory tract infections.
Should not be administered in severe infections.
G I perforation.
37. USTEKINUMAB
Ustekinumab is a human immunoglobulin (Ig) G1
kappa monoclonal antibody directed against
interleukin(IL)-12 and IL-23, which are cytokines
that are involved in immune and inflammatory
responses.
38. Dosing and Uses-
Dosage Forms & Strengths
injectable solution for SC
• 45mg/0.5mL (prefilled syringe or single-dose vial)
• 90mg/mL (prefilled syringe)
injectable solution for IV infusion
• 130mg/26mL (5mg/mL) single-dose vial
39. Uses
Plaque Psoriasis
Indicated for moderate to severe plaque psoriasis in patients who are candidates for
phototherapy or systemic therapy
Psoriatic Arthritis
Indicated for adults with active psoriatic arthritis alone or in combination with
methotrexate
Crohn’s Disease
Indicated for adults with moderately to severely active Crohn disease
Ulcerative Colitis
Indicated for adults with moderately to severely active ulcerative colitis
41. Secukinumab(Cosentyx)
It is a human IgG1κ monoclonal antibody that binds to the
interleukin (IL)-17A.
IL-17 is a group of proinflammatory cytokines released by cells of
the immune system and and exist in higher levels in many immune
conditions associated with chronic inflammation.
42.
43. Dosing and uses
Dosage Forms & Strengths
lyophilized powder for reconstitution
• 150mg/vial
solution for injection
• 150mg/prefilled syringe
• 150mg/Sensoready pen
44. Uses
Plaque Psoriasis
Indicated for treatment of moderate to severe plaque psoriasis in adults who
are candidates for systemic therapy or phototherapy.
Psoriatic Arthritis
Indicated for active psoriatic arthritis (PsA) in adults
For PsA patients with coexistent moderate to severe plaque psoriasis, use
dosage and administration for plaque psoriasis.
Ankylosing Spondylitis
Indicated for adults with active ankylosing spondylitis.
Non-radiographic Axial Spondyloarthritis
Indicated for active non-radiographic axial spondylarthritis with objective signs
of inflammation.
46. Belimumab( Benlysta)
Belimumab is a B-lymphocyte stimulator (BLyS)-specific
inhibitor that indirectly inhibits B cell survival.
it is a fully human recombinant IgG1λ monoclonal
antibody .
It is the first biological treatment approved for the
indication of SLE.
47. Mechanism of action
Belimumab selectively binds to soluble
human B lymphocyte stimulator protein
(BLyS) so that BLyS is unable to bind to
receptors on B lymphocytes.
The binding of BLyS to its receptor is
essential for the survival of B lymphocytes.
Consequently, belimumab reduces B-cell
mediated immunity and the autoimmune
response.
48. Dosing and Uses
Dosage Forms & Strengths
injection, lyophilized powder for reconstitution
• 120mg/vial
• 400mg/vial
SC solution
• 200mg/mL single-dose, prefilled syringe or autoinjector
49. Uses
Systemic Lupus Erythematosus
Indicated for active, autoantibody-positive systemic lupus
erythematosus (SLE) in patients who are receiving standard
therapy.
Lupus Nephritis
Indicated for active lupus nephritis in patients who are receiving
standard therapy.
50. Adverse effects
• nausea
• diarrhea
• fever
• stuffy or runny nose
• sore throat
• cough (bronchitis)
• leg or arm pain
• headache (migraine)
• urinary tract infection
• decreased white blood cell count (leukopenia)
• vomiting
• stomach pain
• injection site reactions (if medication is given under the skin)
51. Ocrelizumab(Ocrevus)
It is a recombinant humanized monoclonal IgG1 antibody
that selectively targets the B lymphocytes that express the
CD20 antigen.
Ocrelizumab promotes antibody-dependent cellular cytotoxicity
and complement-mediated cell lysis.
Another mechanism is apoptosis.
52. Dosing and uses
Dosage Forms & Strengths
solution for injection
• 30mg/mL (10mL single-dose vial)
Multiple Sclerosis
Indicated for adults with relapsing or primary progressive forms of multiple
sclerosis.
