Bevacizumab: Difference between revisions

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<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Rivastigmine/Riv/1" align="right" caption="Rivastigmine, also known as Exelon"/>
<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="" align="right" caption="Bevacizumab, also known as Avastin"/>
===Better Known as: Exelon===
===Better Known as: Avastin===
* Marketed By: Novartis<br />
* Marketed By: Genentech & Roche<br />
* Major Indication: [[Alzheimer's Disease]]<br />
* Major Indication: Colorectal [[Cancer]]<br />
* Drug Class: [[Acetylcholinesterase]] Inhibitor
* Drug Class: [[VEGF]] Inhibitor - [[Monoclonal Antibody]]
* Date of FDA Approval (Patent Expiration): 2007 (<br />
* Date of FDA Approval (Patent Expiration): 2004 (
* 2006 Sales: $220 Million<ref>Irena Melnikova, Therapies for Alzheimer's disease, Nature Reviews Drug Discovery 6, 341-342 (May 2007)</ref>
* 2009 Sales: $4.8 Billion<ref>Irena Melnikova, Therapies for Alzheimer's disease, Nature Reviews Drug Discovery 6, 341-342 (May 2007)</ref>
* Importance: One of the the first treatments for the symptoms of [[Alzheimer's Disease]], although no definitive proof exists as to whether it alters the progression of the disease.  
* Importance: It is one of the best selling [[cancer]] treatments in history. Despite being effective against colorectal cancer, post-approval studies after accelerated approval revealed that Avastin was ineffective in treating breast cancer. Many question the $90,000/year bill to take Avastin when it extends life on average only 10 months.
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information


===Mechanism of Action===
===Mechanism of Action===
Rivastigmine is an [[Acetylcholinesterase]] (AChE) inhibitor. It binds to the active site of <scene name='Rivastigmine/Acetylcholinesterase/1'>AChE</scene>, utilizing many of the same residues which bind and break down acetylcholine. By inhibiting AChE, the important neurotransmitter, [[acetylcholine]], is degraded at a slower rate, helping reverse the marked decrease in neuronal function evident in [[Alzheimer's Disease]] patients. Rivastigmine is rapidly metabolized into its principal components (carbamyl and NAP moieties) which are powerful Acetylcholine inhibitors. These components primarily <scene name='Rivastigmine/Bound/1'>primarily interact with residues</scene> GLy 117, Gly 118, Gly 119 Ala 201, Trp 233, Phe 290, Trp 84, Phe 330, His 440, & Phe 288 in tightly binding to the AChE binding site via pi stacking and hydrogen bond interactions. Rivastigmine outcompetes acetylcholine for the active site of AChE, inhibiting the esterase<ref>PMID:11888271</ref>


===Pharmacokinetics===
===Pharmacokinetics===
{| class="wikitable" border="1" width="30%" style="text-align:center"
{| class="wikitable" border="1" width="30%" style="text-align:center"
|-
|-
!  colspan="2" align="center"| VEGF Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]]
!  colspan="2" align="center"| VEGF Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]]<ref>PMID:17093010</ref>
|-
|-
! Parameter
! Parameter
Line 25: Line 23:
|-
|-
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)  
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)  
! 248.5
! 284000
|-
|-
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Bevacizumab]]
! 100
|-
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
! [[Bevacizumab]]
|-
|-
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (days)
! 15.3
! 20
|-
|-
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ug/ml/hr)
! 133208
! 97488
|-
|-
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
! [[Bevacizumab]]
! .9
|-
|-
! [[Pharmaceutical_Drugs#Clearance_.28Cl.29|Clearance]] (L/h)
! [[Pharmaceutical_Drugs#Clearance_.28Cl.29|Clearance]] (L/h)
! .0086
! .0096
|-
|-
! Dosage (mg/kg)
! Dosage (mg/kg)
! 10
! 10
|-
! Metabolism
! [[Bevacizumab]]
|}
|}


Revision as of 14:35, 6 December 2010

Bevacizumab, also known as Avastin

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Better Known as: Avastin

  • Marketed By: Genentech & Roche
  • Major Indication: Colorectal Cancer
  • Drug Class: VEGF Inhibitor - Monoclonal Antibody
  • Date of FDA Approval (Patent Expiration): 2004 (
  • 2009 Sales: $4.8 Billion[1]
  • Importance: It is one of the best selling cancer treatments in history. Despite being effective against colorectal cancer, post-approval studies after accelerated approval revealed that Avastin was ineffective in treating breast cancer. Many question the $90,000/year bill to take Avastin when it extends life on average only 10 months.
  • The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information

Mechanism of Action

Pharmacokinetics

VEGF Inhibitor Pharmacokinetics[2]
Parameter Bevacizumab
Tmax (hr) 5.17
Cmax (ng/ml) 284000
Bioavailability (%) 100
T1/2 (days) 20
AUC (ug/ml/hr) 97488
IC50 (nM) .9
Clearance (L/h) .0096
Dosage (mg/kg) 10


References

  1. ↑ Irena Melnikova, Therapies for Alzheimer's disease, Nature Reviews Drug Discovery 6, 341-342 (May 2007)
  2. ↑ Garnier-Viougeat N, Rixe O, Paintaud G, Ternant D, Degenne D, Mouawad R, Deray G, Izzedine H. Pharmacokinetics of bevacizumab in haemodialysis. Nephrol Dial Transplant. 2007 Mar;22(3):975. Epub 2006 Nov 8. PMID:17093010 doi:10.1093/ndt/gfl664


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David Canner, Joel L. Sussman, Michal Harel, Alexander Berchansky
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