Basic Information Experimental Physicochemical Property Pharmacokinetic/Toxicokinetic Property Maximum Dosage Drug Property Radar Chart

Basic Information

Drug ID DDPD00864 ...
Drug Name Tacrolimus
Molecular Weight 804.0182
Molecular Formula C44H69NO12
CAS Number 104987-11-3
SMILES CO[C@@H]1C[C@@H](CC[C@H]1O)\C=C(/C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@H](C[C@@H](C)C\C(C)=C\[C@@H](CC=C)C(=O)C[C@H](O)[C@H]1C)OC
External Links
DRUGBANK DB00864
T3DB T3D4732
PubChem Compound 445643
PDR 1331
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Log P 3.3 - 3.3 - DRUGBANK
Melting Point 126.0 ℃ 126 ℃ DRUGBANK

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
Bioavailability 17.0 % 17±10 % PO, oral; adults; renal transplant; DRUGBANK
Bioavailability 22.0 % 22±6 % PO, oral; adults; liver transplant; DRUGBANK
Bioavailability 18.0 % 18±5 % PO, oral; normal,healthy; DRUGBANK
Bioavailability 31.0 % 31±24 % PO, oral; Children; DRUGBANK
Bioavailability 25.0 % 25±10 % The Pharmacological Basis of Therapeutics
C Max 31.2 ng/ml 31.2±10.1 ng/ml Oral single dose; adults; normal,healthy; The Pharmacological Basis of Therapeutics
T Max 1.4 h 1.4±0.5 h Oral single dose; adults; normal,healthy; The Pharmacological Basis of Therapeutics
Clearance 0.0400 L/h/kg 0.04 L/h/kg intravenous injection, IV; normal,healthy; DRUGBANK
Clearance 0.17 L/h/kg 0.172±0.088 L/h/kg PO, oral; normal,healthy; DRUGBANK
Clearance 0.0830 L/h/kg 0.083 L/h/kg intravenous injection, IV; renal transplant; patients; adults; DRUGBANK
Clearance 0.0530 L/h/kg 0.053 L/h/kg intravenous injection, IV; liver transplant; patients; adults; DRUGBANK
Clearance 0.0510 L/h/kg 0.051 L/h/kg intravenous injection, IV; heart transplant; patients; adults; DRUGBANK
Clearance 0.14 L/h/kg 0.138±0.071 L/h/kg liver transplant; pediatric patients; DRUGBANK
Clearance 0.12 L/h/kg 0.12±0.04 L/h/kg renal transplant; pediatric patients; DRUGBANK
Clearance 0.0380 L/h/kg 0.038±0.014 L/h/kg intravenous injection, IV; RD, renal impairment, Renal disease，including uremia; patients; DRUGBANK
Clearance 0.0420 L/h/kg 0.042±0.02 L/h/kg intravenous injection, IV; mild hepatic impairment; DRUGBANK
Clearance 0.0340 L/h/kg 0.034±0.019 L/h/kg PO, oral; mild hepatic impairment; DRUGBANK
Clearance 0.0170 L/h/kg 0.017±0.013 L/h/kg intravenous injection, IV; severe hepatic impairment; DRUGBANK
Clearance 0.0160 L/h/kg 0.016±0.011 L/h/kg PO, oral; severe hepatic impairment; DRUGBANK
Clearance 0.0540 L/h/kg 0.90±0.29 ml/min/kg liver transplant; patients; hydrolysis; Hepatic cirrhosis, cirr → ;RD, renal impairment, Renal disease，including uremia → ; The Pharmacological Basis of Therapeutics
Clearance 0.0420 L/h/kg 0.7 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 2.6 L/kg 2.6±2.1 L/kg liver transplant; pediatric patients; DRUGBANK
Volume of Distribution 1.1 L/kg 1.07±0.20 L/kg intravenous injection, IV; RD, renal impairment, Renal disease，including uremia; patients; DRUGBANK
Volume of Distribution 3.1 L/kg 3.1±1.6 L/kg intravenous injection, IV; mild hepatic impairment; patients; DRUGBANK
Volume of Distribution 3.7 L/kg 3.7±4.7 L/kg PO, oral; mild hepatic impairment; patients; DRUGBANK
Volume of Distribution 3.9 L/kg 3.9±1.0 L/kg intravenous injection, IV; severe hepatic impairment; patients; DRUGBANK
Volume of Distribution 3.1 L/kg 3.1±3.4 L/kg PO, oral; severe hepatic impairment; patients; DRUGBANK
Volume of Distribution 0.91 L/kg 0.91±0.29 L/kg liver transplant; patients; Hepatic cirrhosis, cirr ↑ ;RD, renal impairment, Renal disease，including uremia → ;renal transplant ↑ ; The Pharmacological Basis of Therapeutics
Volume of Distribution 1.2 L/kg 1.2 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 35.0 h 35 h elimination half-life; normal,healthy; adults; DRUGBANK
Half-life 19.0 h 19 h elimination half-life; renal transplant; patients; DRUGBANK
Half-life 12.0 h 12 h elimination half-life; liver transplant; patients; DRUGBANK
Half-life 24.0 h 24 h elimination half-life; heart transplant; patients; DRUGBANK
Half-life 11.5 h 11.5±3.8 h elimination half-life; pediatric patients; liver transplant; DRUGBANK
Half-life 10.2 h 10.2±5.0(3.4-25) h elimination half-life; pediatric patients; renal transplant; DRUGBANK
Half-life 12.0 h 12±5 h liver transplant; patients; RD, renal impairment, Renal disease，including uremia → ;Hepatic cirrhosis, cirr ↑ ; The Pharmacological Basis of Therapeutics
Half-life 26.0 h 26 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity LD50 164.0 mg/kg 134-194 mg/kg Rattus, Rat; DRUGBANK
Toxicity LD50 164.0 mg/kg 134-194 mg/kg Rattus, Rat; T3DB
Eliminate Route 92.6 % 92.6±30.7 % Faeces excretion; intravenous injection, IV; DRUGBANK
Eliminate Route 2.3 % 2.3±1.1 % Urinary excretion; intravenous injection, IV; DRUGBANK
Eliminate Route 1.0 % <1 % Urinary excretion; human, homo sapiens; Unchanged drug; DRUGBANK
Eliminate Route 1.0 % <1 % Urinary excretion; Unchanged drug; The Pharmacological Basis of Therapeutics
Protein Binding 99.0 % ~99 % plasma proteins; human, homo sapiens; DRUGBANK
Protein Binding 87.0 % 75-99 % liver transplant; human, homo sapiens; The Pharmacological Basis of Therapeutics

Maximum Dosage

Property Name Property Value Unit Raw Value Raw Unit Annotation Brand Name Component Reference
Max dose for children 2.0 application/day 2 application/day skin/dermal Prograf tacrolimus PDR
Max dose for adolescents 2.0 application/day 2 application/day skin/dermal Prograf tacrolimus PDR
Max dose for adults 2.0 appLication/day 2 appLication/day skin/dermal Prograf tacrolimus PDR
Max dose for elderly 2.0 application/day 2 application/day skin/dermal Prograf tacrolimus PDR

Drug Property Radar Chart

...

Note: Center: Q1-1.5*IQR, Edge: Q3+1.5*IQR; Q1: Quantile 1, Q3: Quantile 3, IQR: Q3-Q1