Tyrosine Kinase Inhibitor Pharmacokinetics

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{| class="wikitable" border="1" width="40%" style="text-align:center"
{| class="wikitable" border="1" width="40%" style="text-align:center"
|-
|-
-
! colspan="16" align="center"| Cyclooxygenase Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]]
+
! colspan="16" align="center"| Tyrosine Kinase Inhibitor [[Pharmacokinetics]] <ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref><ref>R. Khosravan, et al. General Poster Session, Developmental Therapeutics: Cytotoxic Chemotherapy, J Clin Oncol 26: 2008 (May 20 suppl; abstr 2578)</ref><ref>PMID:16133532</ref><ref>PMID:20821331</ref><ref>PMID:20717111</ref>
|-
|-
! Parameter
! Parameter
-
! Ibuprofen (Advil)
+
! [[Sunitinib]] (Sutent)
-
! Naproxen (Aleve)
+
! [[Sorafenib]] (Nexavar)
-
! Flurbiprofen (Ansaid)
+
! [[Erlotinib]] <br/>(Tarceva)
-
! Acetylsalicylic Acid (Aspirin)
+
! [[Gefitinib]] <br/>(Iressa)
-
! Valdecoxib (Bextra)
+
! [[Lapatinib]] <br/>(Tykerb)
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|-
|-
-
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
+
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
-
! Ibuprofen (Advil)
+
! 8
-
! Naproxen (Aleve)
+
! 8.3
-
! Flurbiprofen (Ansaid)
+
! 2.0
-
! Acetylsalicylic Acid (Aspirin)
+
! 5.4
-
! Valdecoxib (Bextra)
+
! 4
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|-
|-
-
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
+
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
-
! Ibuprofen (Advil)
+
! 24.6
-
! Naproxen (Aleve)
+
! 460
-
! Flurbiprofen (Ansaid)
+
! 69.6
-
! Acetylsalicylic Acid (Aspirin)
+
! 130
-
! Valdecoxib (Bextra)
+
! 115
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|-
|-
-
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
+
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
-
! Ibuprofen (Advil)
+
! Variable
-
! Naproxen (Aleve)
+
! 29-49
-
! Flurbiprofen (Ansaid)
+
! 99
-
! Acetylsalicylic Acid (Aspirin)
+
! 59
-
! Valdecoxib (Bextra)
+
! Variable
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|-
|-
-
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
+
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
-
! Ibuprofen (Advil)
+
! 95
-
! Naproxen (Aleve)
+
! 99
-
! Flurbiprofen (Ansaid)
+
! 93
-
! Acetylsalicylic Acid (Aspirin)
+
! 90
-
! Valdecoxib (Bextra)
+
! 99
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|-
|-
-
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
+
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
-
! Ibuprofen (Advil)
+
! 83
-
! Naproxen (Aleve)
+
! 29
-
! Flurbiprofen (Ansaid)
+
! 9.4
-
! Acetylsalicylic Acid (Aspirin)
+
! 26.9
-
! Valdecoxib (Bextra)
+
! 9.6
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|-
|-
-
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
+
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
-
! Ibuprofen (Advil)
+
! 1921
-
! Naproxen (Aleve)
+
! 11040
-
! Flurbiprofen (Ansaid)
+
! 20577
-
! Acetylsalicylic Acid (Aspirin)
+
! 3850
-
! Valdecoxib (Bextra)
+
! 1429
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
-
|-
+
-
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
+
-
! Ibuprofen (Advil)
+
-
! Naproxen (Aleve)
+
-
! Flurbiprofen (Ansaid)
+
-
! Acetylsalicylic Acid (Aspirin)
+
-
! Valdecoxib (Bextra)
+
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
-
|-
+
-
! [[Pharmaceutical_Drugs#Clearance_.28Cl.29|Clearance]] (L/h)
+
-
! Ibuprofen (Advil)
+
-
! Naproxen (Aleve)
+
-
! Flurbiprofen (Ansaid)
+
-
! Acetylsalicylic Acid (Aspirin)
+
-
! Valdecoxib (Bextra)
+
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|-
|-
! Dosage (mg)
! Dosage (mg)
-
! Ibuprofen (Advil)
+
! 50
-
! Naproxen (Aleve)
+
! 50
-
! Flurbiprofen (Ansaid)
+
! 150
-
! Acetylsalicylic Acid (Aspirin)
+
! 250
-
! Valdecoxib (Bextra)
+
! 100
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|-
|-
! Metabolism
! Metabolism
-
! Ibuprofen (Advil)
+
! Hepatic (CYP3A4)
-
! Naproxen (Aleve)
+
! Hepatic (CYP3A4)
-
! Flurbiprofen (Ansaid)
+
! Hepatic - (CYP3A4)
-
! Acetylsalicylic Acid (Aspirin)
+
! Hepatic - (CYP3A4)
-
! Valdecoxib (Bextra)
+
! Hepatic - (CYP3A4)
-
! Celecoxib (Celebrex)
+
-
! Sulindac (Clinoril)
+
-
! Oxaprozin (Daypro)
+
-
! Piroxicam (Feldene)
+
-
! Nabumetone (Relafen)
+
-
! Acetaminophen (Paracetamol)
+
-
! Mefanamic Acid (Ponstel)
+
-
! Ketorolac (Toradol)
+
-
! Rofecoxib (Vioxx)
+
-
! Diclofenac (Voltaren)
+
|}
|}

Revision as of 13:16, 9 December 2010

Tyrosine Kinase Inhibitor Pharmacokinetics [1][2][3][4][5]
Parameter Sunitinib (Sutent) Sorafenib (Nexavar) Erlotinib
(Tarceva) 		Gefitinib
(Iressa) 		Lapatinib
(Tykerb)
Tmax (hr) 8 8.3 2.0 5.4 4
Cmax (ng/ml) 24.6 460 69.6 130 115
Bioavailability (%) Variable 29-49 99 59 Variable
Protein Binding (%) 95 99 93 90 99
T1/2 (hr) 83 29 9.4 26.9 9.6
AUC (ng/ml/hr) 1921 11040 20577 3850 1429
Dosage (mg) 50 50 150 250 100
Metabolism Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic - (CYP3A4) Hepatic - (CYP3A4) Hepatic - (CYP3A4)

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David Canner

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