Transcript Slide 1

Biologics: Indications and
Approaches
Russell D. Cohen, MD, AGAF, FACG
Professor of Medicine, Pritzker School of Medicine
Director IBD Center
Co-Director Advanced IBD Fellowship
Disclosures
•
Speaker’s Bureau:
– Abbvie, Entera Health, Salix Pharmaceuticals, Shire PLC
•
Consultant / Advisory/ Data Safety Monitoring/ Scientific Advisory Board:
– Abbvie, Cellgene, Elan Pharmaceuticals, Entera Health, Hospira, Janssen
(Johnson & Johnson / Centocor), Prometheus Laboratories, Salix Pharmaceuticals,
Sandoz Biopharmaceuticals, Santarus, Shire pLC, Takeda, UCB Pharma
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“The Tale of Two Families”
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FAMILY #1: The Anti-TNF’s
FDA- Approved Therapies
Generic
Branded
Crohn’s Disease
Ulcerative Colitis
Adalimumab
Humira®
+
+
Certolizumab
Cimzia®
+
Golimumab
Simponi®
Infliximab
Remicade®
+
+
+
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Comparison of anti-TNF Agents
Chimeric
monoclonal
antibody
Humanized Fab’
Human recombinant
fragment
receptor/Fc fusion protein
Human
recombinant
antibody
Humanized
monoclonal
antibody
VL
Fab
VH
Receptor
CDR
Ck
CH1
Constant 2
Fc
Constant 3
Infliximab
Mouse
Human
CDP571
Adalimumab
Golimumab
CDR = Complementarity-determining region
PEG = Polyethylene glycol
Etanercept
•PEG •PEG
Certolizumab pegol
Hanauer, Rev Gastroenterol Disord 2004; 4 (supp 3): S18-24
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Benefits vs. Drawbacks: Anti-TNF’s
• Benefits
• Work fast.
• Work very well in many
patients.
• Dosed only every 2 weeks –
2 months.
• Contain no steroids; so have
no steroid side-effects.
• Long-term safety profile
excellent.
• Drawbacks
• Given IV or by shot only.
• May become allergic or
ineffective if stop and then
restart later.
• Internet-hype over very
very rare potential risk of
lymphoma and potential
increased risk of skin
cancers
The benefits far outweigh the extremely rare risks in
the vast majority of patients.
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FDA Indication: Adalimumab in Crohn’s
Disease
Adult & Pediatric Patients
• Reducing signs and symptoms
• Inducing and maintaining clinical
• Moderately to severely active disease who have had an
inadequate response to conventional therapy
– Pediatrics: specifies “corticosteroids or immumodulators such as
azathioprine, 6-mercaptopurine, or methotrexate.”
Adult Patients
• Reducing signs and symptoms and inducing clinical remission in
patients if they have also lost response to or are intolerant to
http://www.rxabbvie.com/pdf/humira.pdf Accessed 11/9/2014
infliximab
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FDA Indication: Adalimumab in
Ulcerative Colitis
Adult Patients
• Inducing and maintaining clinical remission
• Moderately to severely active disease who have had an
inadequate response to immunosuppressants
• “such as corticosteroids, azathioprine, or 6-mercaptopurine
(6-MP)”
• “The effectiveness of adalimumab has not been established in
patients who have lost response to or were intolerant to TNF
blockers.”
http://www.rxabbvie.com/pdf/humira.pdf Accessed 11/9/2014
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Adalimumab Dosing (CD and UC)
• Load
– Week 0: 160mg sc (syringe or pen)
– Week 2: 80mg sc (syringe or pen)
SC ONLY
• More convenient
• Less compliant?
• Self-Medicating?
• Maintenance
– Starting @ Week 4: 40mg sc every other week.
• If lose response:
– Increase to qweekly dosing.
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Adalimumab: Dosing Issues
1. Use of trough levels to optimize therapy
2. Increase dose: 40 q week or 80 q2 weeks
3. Best outcomes with combination therapy
4. ? If doses over 80mg should be used.
5. High dose loading in severe disease?
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FDA Indication: Certolizumab in Crohn’s
Disease
Adult Patients
• Reducing signs and symptoms
• Maintaining clinical response
• Moderately to severely active disease who have had an
inadequate response to conventional therapy
http://www.cimzia.com/assets/pdf/Prescribing_Information.pdf Accessed 11/9/2014
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Certolizumab Pegol Dosing (CD)
SC ONLY
• Load
• Week 0: 400 mg sc
• Week 2: 400 mg sc
• Maintenance
1.Lyophylized drug:
Mixed and Administered
by health care professional
• +/- convenient
• More compliant?
• Less Self-Medicating?
• Preferred if Medicare
2. Prefilled syringe:
•
More convenient
• Starting @ Week 4: 400 mg sc every 4 weeks
• If lose response:
– Give an extra dose of 400 mg 2 weeks after last dose
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Certolizumab Pegol: Dosing Issues
1. Use of trough levels to optimize therapy ? (N/A)
2. Increase dose to 400 q2 weeks: effective?
3. Best outcomes with combination therapy
4. High dose loading in severe disease?
5. Choose the lyophilized version for Medicare patients
(Medicare pays for injectables if administered by a health
care professional)
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FDA Indication: Golimumab in UC
Adult Patients
• Inducing and maintaining clinical response
• Inducing clinical remission
• Achieving and sustaining clinical remission in induction
responders
• Improving endoscopic appearance of the mucosa during
induction
• Moderate to severe ulcerative colitis with an inadequate
response or intolerant to prior treatment or requiring
continuous steroid therapy
http://www.simponi.com/shared/product/simponi/prescribing-information.pdf Accessed 11/9/2014
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Golimumab Dosing (UC)
• Load
– Week 0: 200 mg sc (syringe or pen)
– Week 2: 100 mg sc (syringe or pen)
SC ONLY
• More convenient
• Less compliant?
• Self-Medicating?
• Maintenance
– Starting @ Week 4: 100mg sc every 4 weeks.
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Golimumab: Dosing Issues
1. Use of trough levels to optimize therapy? (N/A)
2. Increase dose?
3. Best outcomes with combination therapy (anticipated)
4. ? If doses over 200 mg should be used.
5. High dose loading in severe disease?
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FDA Indication: Infliximab in Crohn’s
Disease
Adult & Pediatric Patients
• Reducing signs and symptoms
• Inducing and maintaining clinical
• Moderately to severely active disease who have had an
inadequate response to conventional therapy
Adult Patients
• Reducing the number of draining enterocutaneous and
rectovaginal fistulas
• Maintaining fistula closure
http://www.remicade.com/shared/product/remicade/prescribing-information.pdf Accessed 11/9/2014
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FDA Indication: Infliximab in Ulcerative
Colitis
Adult & Pediatric Patients
• Reducing signs and symptoms
• Inducing and maintaining clinical remission
• Moderately to severely active disease who have had an
inadequate response to conventional therapy
Adult Patients
• Inducing and maintaining mucosal healing
• Eliminating corticosteroid use
http://www.remicade.com/shared/product/remicade/prescribing-information.pdf Accessed 11/9/2014
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Infliximab: Dosing (Crohn’s and UC)
• Load:
• Week 0: 5mg/kg IV
• Week 2: 5mg/kg IV
• Week 6: 5mg/kg IV
IV ONLY
• Less convenient
• More compliant
• Maintenance:
• Starting @ Week 14: 5 mg/kg IV q 8 weeks.
• If lose response:
• Increase dose up to 10mg/kg or decrease dosing
interval.
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Infliximab: Dosing Issues
1. Use of trough levels to optimize therapy
2. ? If should increase dose or decrease duration between
infusions
3. Best outcomes with combination therapy
4. ? If doses over 10mg/kg should be used
5. Aggressive loading in severe disease?
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Combination Therapy: Superior Efficacy in
Crohn’s
Anti-Infliximab
Antibodies:
Mono: 14%
Combo: 1%
P<0.001 vs. aza
P=0.022 vs. ifx
P<0.001 vs. aza
P=0.055 vs. ifx
Columbel JF et al. N Engl J Med 2010;362:1383-95.
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Combination Therapy: Superior Efficacy in
Ulcerative Colitis
Anti-Infliximab
Antibodies:
Mono: 14%
Combo: 1%
Panaccione et al. Gastroenterology 2014;146:392-400 e3
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Best Outcomes With Combination Therapy
(Biologics + Immunosuppressant)
Infliximab + Azathioprine:
Crohn’s Disease (SONIC Trial) 1
Ulcerative Colitis (UC-SUCCESS Trial) 2
Is the same true for adalimumab?
When should thiopurine be started?
Should thiopurines be at therapeutic doses?
Should biologics be at therapeutic doses?
1
2
Columbel JF et al. N Engl J Med 2010;362:1383-95.
Panaccione et al. Gastroenterology 2014;146:392-400.
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FAMILY #2: The Anti-Integrin Antibodies
FDA- Approved Therapies
Generic
Branded
Crohn’s Disease
Natalizumab
Tysabri®
+
Vedolizumab
Entyvio®
+
Ulcerative Colitis
+
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FDA Indication: Natalizumab in Crohn’s
Disease
Adult Crohn’s Disease:
I.
II.
III.
Inducing and Maintaining Clinical Response
Inducing and Maintaining Clinical Remission
Moderate – to – Severe active Crohn’s Disease
I.
IV.
V.
With evidence of inflammation
Inadequate response to, or are unable to tolerate
conventional CD therapies and inhibitors of TNF-α.
In CD, should not be used in combination with
immunosuppressants or inhibitors of TNF-α.
FDA Prescribing Information : v 05/2014
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Natalizumab: Dosing (CD)
• Verify JC virus “-”
• No Load
• Standard Dosing Regimen
IV ONLY
“CD-TOUCH” Program
• Less convenient
• More compliant?
• 300 mg IV every 4 weeks
• No other immunomodulators allowed; taper
prednisone
• If no response or lose response:
• Stop therapy
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Natalizumab: Dosing Issues
1. Verify JC virus “-” prior to starting
2. Recheck JC virus q6-12 months
- Stop therapy if converts to JC “+”
3. Verify drug working by month 6; otherwise stop.
4. Can check drug level if ? of low level / likely antibodies
5. If JC virus status “-” should one be “allowed to”:
• Use concomitant immunomodulators?
• Dose increase ?
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FDA Indication: Vedolizumab in Crohn’s
Disease
Adult Crohn’s Disease:
I.
II.
Moderate – to – Severe active Crohn’s Disease
Inadequate response with, lost response to, or intolerant to either
a.
b.
c.
III.
Anti- TNF blocker
Immunomodulator
Corticosteroids (or dependent)
Outcomes:
a.
b.
c.
Achieving clinical response
Achieving clinical remission
Achieving corticosteroid-free remission
FDA Prescribing Information : v 05/2014
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FDA Indication: Vedolizumab in
Ulcerative Colitis
Adult Ulcerative Colitis:
I.
II.
Moderate – to – Severe active UC
Inadequate response with, lost response to, or intolerant to either
a.
b.
c.
III.
Anti- TNF blocker
Immunomodulator
Corticosteroids (or dependent)
Outcomes:
a.
b.
c.
d.
Inducing and maintaining clinical response
Inducing and maintaining clinical remission
Improving endoscopic appearance of the mucosa
Achieving corticosteroid-free remission
FDA Prescribing Information : v 05/2014
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Vedolizumab: Dosing (Crohn’s and UC)
• Load:
• Week 0: 300 mg IV
• Week 2: 300 mg IV
• Week 6: 300 mg IV
IV ONLY
• Less convenient
• More compliant
• Maintenance:
• Starting @ Week 14: 300 mg IV q 8 weeks.
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Vedolizumab: Dosing Issues
1. Use of trough levels to optimize therapy ? (N/A)
2. Decrease time between maintenance infusions to q4
weeks if needed?
3. Best outcomes with combination therapy ?
4. Overlap with other induction agents
•
•
•
Steroids √
Calcineurin inhibitors ?
Anti-TNF’s ?
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Vedolizumab Blocks α4β7 Integrin
Inflammatory
Cytokines
Anti-a4
a4b1
a4b7
T cell
MAdCAM-1
Lanzarotto F, et al. Drugs. 2006;66(9):1179-1189.
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Vedolizumab: Induction in UC
100%
GEMINI I
Primary Analysis: Week 6
75%
P<0.001
50%
25%
P=0.001
47.1%
Vedolizumab
40.9%
25.5%
P=0.001
Placebo
24.8%
16.9%
5.4%
0%
Clinical Response
Clinical Remission
Mucosal Healing
Feagan BG et al. N Engl J Med 2013;369(8):699-710),.
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Vedolizumab: Maintenance in UC
100%
GEMINI I
Vedolizumab q 4w
Week 52
Vedolizumab q 8w
Placebo
P<0.001 for either drug group vs.
placebo
75%
P = 0.01
v.
placebo
56.6%
52.0%
50%
56.0%
44.8%
41.8%
51.6%
45.2%
31.4%
25%
23.8%
15.9%
19.8%
13.9%
0%
Clinical Response
Clinical Remission Steroid-Free Remission Mucosal Healing
Feagan BG et al. N Engl J Med 2013;369(8):699-710),.
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Vedolizumab: Induction in Crohn’s
100%
GEMINI II
Primary Analysis: Week 6
75%
Vedolizumab
50%
P = 0.23
31.4%
25%
Placebo
25.7%
P = 0.02
14.5%
6.8%
0%
Clinical Response
Clinical Remission
Sandborn et al. N Engl J Med 2013;369(8):711-721.
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Vedolizumab: Maintenance in Crohn’s
100%
GEMINI II
Vedolizumab q 4w
Week 52
Vedolizumab q 8w
Placebo
75%
P=0.005
50%
P=0.004
45.5% 43.5%
30.1%
P<0.001
36.4% 39.0%
P=0.04
28.8%
21.6%
25%
P=0.02
31.7%
15.9%
0%
Clinical Response
P values vs. placebo
Clinical Remission
Steroid-Free Remission
Feagan BG et al. N Engl J Med 2013;369(8):699-710),.
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Dosing Biologics By Trough Levels
“+”
• Higher Response Rates
• Higher Endoscopic
Healing Rates
• Lower Hospitalization
Rates
• Lower Surgical Rates
• Cost-Effective
GI Meetings
2013-4
“–”
• Extremely Expensive
• Trouble Getting
Insurance Coverage
• Requires Repeat Testing
• Slow Turn-Around Time
• Hard to Interpret
Results from Different
Labs
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Ongoing Debates With Biologics
1. Earlier Use of anti-TNF’s ?
2. Monotherapy vs. Combination therapy ?
3. Withdrawal of Therapies ?
Answers to These Dilemmas:
Tomorrow’s Program !
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