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

Basic Information

Drug ID DDPD00091 ...
Drug Name Cyclosporine
Molecular Weight 1202.635
Molecular Formula C62H111N11O12
CAS Number 59865-13-3
SMILES CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O)C(C)C
External Links
DRUGBANK DB00091
T3DB T3D3498
PubChem Compound 5284373
PDR 11
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Caco-2 Permeability -6.05 - -6.05 - ADME Research, USCD
Log P 1.4 - 1.4 - https://www.sciencedirect.com/science/article/pii/S0939641116309080
Boiling Point 838.63 ℃ 838.63 ℃ https://www.chemicalbook.com/ChemicalProductProperty_EN_CB5163816.htm
Melting Point 149.5 ℃ 148-151 ℃ https://www.chemicalbook.com/ChemicalProductProperty_EN_CB5163816.htm
pKa 13.32 - 13.32±0.70 - https://www.chemicalbook.com/ChemicalProductProperty_EN_CB5163816.htm

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
Bioavailability 30.0 % 30.0 % PO, oral; DRUGBANK
Bioavailability 38.7 % 38.7 % Capsule, PO, Oral; DRUGBANK
Bioavailability 38.7 % 38.7 % Liquid; DRUGBANK
Bioavailability 28.0 % 28±18 % PO, oral; Drug form; renal transplant; The Pharmacological Basis of Therapeutics
C Max 1101.0 ng/ml 1101±570 ng/ml PO, oral; Drug form; renal transplant; The Pharmacological Basis of Therapeutics
C Max 1333.0 ng/ml 1333±469 ng/ml PO, oral; Drug form; renal transplant; The Pharmacological Basis of Therapeutics
T Max 3.5 h 3.5 h PO, oral; DRUGBANK
T Max 2.9 h 1.8-4.0 h PO, oral; Drug form; renal transplant; The Pharmacological Basis of Therapeutics
T Max 1.8 h 1.5-2 h PO, oral; Drug form; renal transplant; The Pharmacological Basis of Therapeutics
Clearance 1.7 L/h/kg 0.38-3 L/h/kg DRUGBANK
Clearance 22.5 L/h ~22.5 L/h Capsule, PO, Oral; DRUGBANK
Clearance 0.34 L/h/kg 5.7(0.6-24) ml/min/kg renal transplant; patients; hydrolysis; Children ↑ ;Elderly ↓ ;Hepatitis, Hep ↓ ;Hepatic cirrhosis, cirr ↓ ;RD, renal impairment, Renal disease，including uremia → ; The Pharmacological Basis of Therapeutics
Clearance 0.45 L/h/kg 7.5 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 6.0 L/kg 4.0-8 L/kg DRUGBANK
Volume of Distribution 4.5 L/kg 4.5(0.12-15.5) L/kg renal transplant; patients; Children ↑ ;Elderly ↓ ; The Pharmacological Basis of Therapeutics
Volume of Distribution 3.3 L/kg 3.3 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 19.0 h ~19(10-27) h terminal half-life; DRUGBANK
Half-life 10.7 h 10.7(4.3-53) h renal transplant; patients; Children ↓ ;Age → ; The Pharmacological Basis of Therapeutics
Half-life 7.3 h 7.3 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity LD50 1480.0 mg/kg 1480.0 mg/kg PO, oral; Rattus, Rat; DRUGBANK
Toxicity LD50 2329.0 mg/kg 2329.0 mg/kg PO, oral; mouse; T3DB
Toxicity LD50 1480.0 mg/kg 1480.0 mg/kg PO, oral; Rattus, Rat; T3DB
Toxicity LD50 1000.0 mg/kg >1000 mg/kg PO, oral; rabbit; T3DB
Toxicity LD50 148.0 mg/kg 148.0 mg/kg intravenous injection, IV; mouse; T3DB
Toxicity LD50 104.0 mg/kg 104.0 mg/kg intravenous injection, IV; Rattus, Rat; T3DB
Toxicity LD50 46.0 mg/kg 46.0 mg/kg intravenous injection, IV; rabbit; T3DB
Toxicity TDLo 12.0 mg/kg 12.0 mg/kg human, homo sapiens; DRUGBANK
Eliminate Route 4.5 % 3-6 % Urinary excretion; DRUGBANK
Eliminate Route 90.0 % 90 % Bile excretion; DRUGBANK
Eliminate Route 1.0 % <1 % Unchanged drug; DRUGBANK
Eliminate Route 1.0 % <1 % Urinary excretion; Unchanged drug; The Pharmacological Basis of Therapeutics
Protein Binding 50.0 % ~50 % serum albumin; DRUGBANK
Protein Binding 34.0 % ~34 % DRUGBANK
Protein Binding 93.0 % 93±2 % The Pharmacological Basis of Therapeutics

Maximum Dosage

Property Name Property Value Unit Raw Value Raw Unit Annotation Brand Name Component Reference
Max dose for adolescents 2.0 drop/day 2 drop/day ophthalmic administration Gengraf Capsules cyclosporine PDR
Max dose for adults 2.0 drop/day 2 drop/day ophthalmic administration Gengraf Capsules cyclosporine PDR
Max dose for geriatric 2.0 drop/day 2 drop/day ophthalmic administration Gengraf Capsules cyclosporine PDR

Drug Property Radar Chart

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