Humira

HUMIRA®
Done by : pharmacist lubna Mohammad
Drug formulation officer at HPI
As a requirement for medicinal chemistry course
22/3/2017

Presentation topics
• Introduction
• Pharmacology
• Uses
• How to use ?
• Side effects
• Related drugs
• References

Introduction
• Humira stands for :human monoclonal anti
body in rheumatoid arthritis .
• Human monoclonal antibody against TNF-
alpha.
• C6428H9912N1694O1987S46.

Introduction
• It binds to (TNFα), which normally binds to
TNFα receptors, leading to the
inflammatory response of autoimmune
diseases. By binding to TNFα, adalimumab
reduces this inflammatory response.
• Humira costs approximately $3,100 per
month, From 2012 to US patent expiry in
2016, Humira led the list of top-selling
pharmaceutical products, and in 2016, it
had $16 billion of global sales.

Introduction
History
• Adalimumab was the first fully human
monoclonal antibody approved by the
U.S. Food and Drug administration.
• Engineered through guided
selection techniques phage display
and was discovered through a
collaboration between BASF
Bioresearch Corporation and
Cambridge Antibody Technology.
• Initially named D2E7.

Mechanism of action
• directly binding to TNF- α molecules in the
blood and diseased tissue.
• blocks its interaction with the p55 and p75 cell
surface TNF receptors.
• lyses surface TNF expressing cells in vitro.
• does not bind or inactivate lymphotoxin (TNF-
beta).
• Adalimumab helps to stop the inflammatory
cycle of psoriatic disease and prevent from
causing the inflammation that result in
psoriasis plaques.

TNF
SIGNAL
Monoclonal Antibody directed against
TNF-alpha: Infliximab (Remicade ®),
Adalimumab (Humira®)
Soluble TNF-Receptors serve as a
balance to TNF
Engineered Soluble TNF Receptor
(Enbrel®)

Uses
• Rheumatoid arthritis
• Adalimumab has been shown to
reduce the signs and symptoms of
moderate to severe rheumatoid
arthritis (RA) in adults. it has been
approved for use alone, or with
methotrexate or similar medicines,
in the U.S. since 2002.

Uses
• Psoriatic arthritis
• In 2003, adalimumab began
undergoing trials for use in treating
psoriasis and psoriatic arthritis.
• Ankylosing spondylitis
• Adalimumab has been shown to
reduce the signs and symptoms
and is approved for treatment of,
ankylosing spondylitis in adults.

Uses
• Crohn’s disease
Adalimumab has been shown to reduce the
signs and symptoms of moderate to severe
Crohn's disease. It has been approved for that
use in the UK since 2009.
• Ulcerative colitis
Adalimumab may be effective and well
tolerated in ulcerative colitis. It has been
approved by the FDA for treatment of
moderate to severe cases in adults.

Uses
• Plaque psoriasis
Adalimumab has been shown to treat moderate to severe chronic plaque
psoriasis in adults who have the condition in many areas of their body
Adalimumab has been shown to be effective therapy when used either
continuously or intermittently in patients with moderate to severe psoriasis.
• Juvenile idiopathic arthritis
Humira in combination with methotrexate is indicated for the treatment of
active polyarticular juvenile idiopathic arthritis, in patients from the age of 2
years who have had an inadequate response to one or more disease-
modifying anti-rheumatic drugs (DMARDs). Humira can be given as
monotherapy in case of intolerance to methotrexate or when continued
treatment with methotrexate is inappropriate it has-been shown to reduce
the signs and symptoms of moderate to severe polyarticular juvenile
idiopathic arthritis in children 4 and older.

How to use ?
• Adalimumab is administered by
subcutaneous injection For most
indications, the maintenance
treatment is an injection every other
week.

Side effects
• Upper respiratory tract infection and
asthma like symptoms, latent infections
such as tuberculosis can be reactivated,
and the immune system may be unable to
fight new infections. This has led to fatal
infections in some patients.
• Hepatitis B reactivation , people who
develop HBV reactivation should stop
Humira and effective anti-viral therapy
with appropriate supportive treatment
should be initiated.

Side effects
• Allergic reactions that might lead to Anaphylaxis
or other serious allergic reactions may also occur.
• Immunosuppression the immune system may be
unable to fight new infections. This has led to fatal
infections in some patients.
• Malignancies and lymphoproliferative disorders In
the controlled portions of clinical trials of TNF-
antagonists, more cases of malignancies including
lymphoma have been observed among patients
receiving a TNF-antagonist compared with control
patients. However, the occurrence was rare

Advantages vs. disadvantages
• Humira (Adalimumab) Advantages:
• Humira (Adalimumab) is injected on the surface of
the body thus hastening it’s absorption into the
body.
• Humira (Adalimumab) has a quick turnaround (one
day up to 2 months) as compared to competition.
• Very rapid onset of action.
• Humira (Adalimumab) Disadvantages:
• Humira (Adalimumab) is available on prescription
only.
• You require a skilled person or training to administer
Humira (Adalimumab).
• Costs approximately $3,100 per month.
• Humira (Adalimumab) side effects some that are
fatal.

Related drugs
• Infliximab (trade names Remicade among others) is a
chimeric monoclonal antibody biologic drug that
works against tumor necrosis factor alpha (TNF-α).
• Certolizumab pegol (CDP870, trade name Cimzia) is a
biologic medication for the treatment of Crohn's
disease, rheumatoid arthritis, psoriatic arthritis and
ankylosing spondylitis.
• Golimumab (CNTO 148) is a human monoclonal
antibody which is used as an immunosuppressive drug
and marketed under the brand name Simponi.
Golimumab targets tumor necrosis factor alpha (TNF-
alpha), a pro-inflammatory molecule.

References
• http://www.aafp.org/afp/2008/1215/p1406.html
• http://www.genengnews.com/the-lists/the-top-15-best-selling-drugs-of-
2016/77900868?utm_medium=newsletter&utm_source=GEN+Daily+News+Highlights&utm_co
ntent=01&utm_campaign=GEN+Daily+News+Highlights_20170307
• https://www.fda.gov/downloads/drugs/drugsafety/ucm088611.pdf
• American College of Rheumatology Subcommittee on Rheumatoid Arthritis Guidelines.
Guidelines for the management of rheumatoid arthritis: 2002 update. Arthritis
Rheum2002;46:328–46.
• OpenUrlCrossRefPubMedWeb of Science
• Brekke OH; Sandlie I (January 2003). "Therapeutic antibodies for human diseases at the dawn of
the twenty-first century". Nat Rev Drug Discov. 2 (1): 52–62. doi:10.1038/nrd984.
PMID 12509759.
• Kempeni J (January 1999). "Preliminary results of early clinical trials with the fully human anti-
TNFα monoclonal antibody D2E7". Ann Rheum Dis. 58 (suppl 1): I70–2.
doi:10.1136/ard.58.2008.i70. PMC 1766582 . PMID 10577977
• Salfeld J, Kaymakçalan Z, Tracey D, Roberts A, Kamen R. Generation of fully human anti-TNF
antibody D2E7. [Abstract]. Arthritis Rheum1998;41 (suppl):S57.
• https://www.ncbi.nlm.nih.gov/pubmed/12884458
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1936294/pdf/tcrm0301-133.pdf
• http://search.proquest.com/openview/321f9bb2c9a8d759fc250b11063bfd7f/1?pq-
origsite=gscholar&cbl=33668
• https://www.omicsgroup.org/journals/analysis-of-the-mechanism-of-action-of-biological-
therapies-in-monotherapy-in-patients-with-rheumatoid-arthritis-beyond-the-adacta-study-
2167-1052.1000141.pdf
• https://www.youtube.com/watch?v=Evsq3I28eHQ
• Siegel, Jay P., M.D., FACP. "Therapeutic Biologic Applications (BLA) – Humira Approval Letter

References
• 12/31/02". Center for Drug Evaluation and Research. Retrieved 2014-02-04.
• "Humira® (Adalimumab) - 2011023-Humira.pdf" (PDF). Retrieved 2014-02-04.
•
• Scheinfeld, N (2003). "Adalimumab (HUMIRA): a review". J Drugs Dermatol. 2 (4): 375–7.
PMID 12884458.
• http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-
_Product_Information/human/000481/WC500050870.pdf
• Maxwell, LJ; Zochling, J; Boonen, A; Singh, JA; Veras, MM; Tanjong Ghogomu, E; Benkhalti
Jandu, M; Tugwell, P; Wells, GA (18 April 2015). "TNF-alpha inhibitors for ankylosing
spondylitis.". The Cochrane database of systematic reviews. 4: CD005468.
doi:10.1002/14651858.CD005468.pub2. PMID 25887212.
•
• Podolsky, Daniel K. (August 2002). "Inflammatory bowel disease". N Engl J Med. 347 (6): 417–
29. doi:10.1056/NEJMra020831. PMID 12167685
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• Jump up ^ Croom, Katherine F; McCormack, Paul L (2009). "Adalimumab". Am J Clin Dermatol.
10 (1): 43–50. doi:10.2165/0128071-200910010-00008. PMID 19170412
• https://academic.oup.com/rheumatology/article-lookup/doi/10.1093/rheumatology/kem356
•

References
• https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=78456
• Jump up to Humira - Full prescribing information
• https://academic.oup.com/rheumatology/article/44/9/1199/2899286/Adalimumab-
induced-asthma
• Karen M. Frank, et al, Investigation of the cause of death in a gene-therapy trial, N Engl
J Med 361:161, July 9, 2009
• http://www.tandfonline.com/doi/abs/10.1517/14740338.4.4.637
• FDA label – http://www.rxabbott.com/pdf/humira_medguide.pdf
• Karen M. Frank, et al, Investigation of the cause of death in a gene-therapy trial, N Engl J Med 361:161, July 9,
2009
•
• "Archived copy". Archived from the original on 2011-07-10. Retrieved 2011-03-06
• https://www.ncbi.nlm.nih.gov/pubmed/27924644
• [Official Website for REMICADE® (infliximab) http://www.remicade.com

References
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• Goel, Niti; Sue Stephens (2010). "Certolizumab pegol". MAbs. 2 (2): 137–147.
doi:10.4161/mabs.2.2.11271. PMC 2840232 . PMID 20190560
•
• Mazumdar, Sohini; David Greenwald (2009). "Golimumab". MAbs. 1 (5): 422–
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• Statement On A Nonproprietary Name Adopted By The USAN Council –
Golimumab
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PMID 16008121

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