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

Basic Information

Drug ID DDPD00481 ...
Drug Name Raloxifene
Molecular Weight 473.583
Molecular Formula C28H27NO4S
CAS Number 84449-90-1
SMILES OC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(OCCN3CCCCC3)C=C2)C2=C(S1)C=C(O)C=C2
External Links
DRUGBANK DB00481
PubChem Compound 5035
PDR 2263
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Log P 5.2 - 5.2 - DRUGBANK
Melting Point 270.0 ℃ 268-272 ℃ MSDS

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
Absorption 60.0 % 60.0 % PO, oral; DRUGBANK
AUC 27.2 ng.h/ml 27.2 ng.h/ml Oral single dose; postmenopausal women; DRUGBANK
AUC 24.2 ng.h/ml 24.2 ng.h/ml Oral multiple dose; postmenopausal women; DRUGBANK
AUC 27.2 ng.h/ml 27.2 ng.h/ml Oral single dose; postmenopausal women; high-fat meal ↑ ; DRUGBANK
AUC 24.2 ng.h/ml 24.2 ng.h/ml Oral multiple dose; postmenopausal women; high-fat meal ↑ ; DRUGBANK
Bioavailability 2.0 % 2.0 % PO, oral; DRUGBANK
Bioavailability 2.0 % 2.0 % PO, oral; The Pharmacological Basis of Therapeutics
C Max 0.50 ng/ml 0.5 ng/ml Oral single dose; postmenopausal women; DRUGBANK
C Max 1.4 ng/ml 1.36 ng/ml Oral multiple dose; postmenopausal women; DRUGBANK
C Max 0.64 ng/ml 0.64 ng/ml Oral single dose; postmenopausal women; high-fat meal ↑ ; DRUGBANK
C Max 1.7 ng/ml 1.7408 ng/ml Oral multiple dose; postmenopausal women; high-fat meal ↑ ; DRUGBANK
C Max 0.50 ng/ml 0.5±0.3 ng/ml PO, oral; The Pharmacological Basis of Therapeutics
T Max 27.7 h 27.7 h Oral single dose; postmenopausal women; DRUGBANK
T Max 32.5 h 32.5 h Oral multiple dose; postmenopausal women; DRUGBANK
T Max 32.1 h 32.132 h Oral single dose; postmenopausal women; high-fat meal ↑ ; DRUGBANK
T Max 37.7 h 37.7 h Oral multiple dose; postmenopausal women; high-fat meal ↑ ; DRUGBANK
T Max 6.0 h 6.0 h PO, oral; The Pharmacological Basis of Therapeutics
Clearance 44.1 L/h/kg 44.1 L/h/kg Total clearance; PO, oral; DRUGBANK
Clearance 50.0 L/h/kg 40-60 L/h/kg Oral multiple dose; DRUGBANK
Clearance 47.4 L/h/kg 47.4 L/h/kg Average clearance; Oral multiple dose; normal,healthy; postmenopausal women; hepatopathy，LD ↓ ; DRUGBANK
Clearance 44.1 L/h/kg 735±338 ml/min/kg apparent clearance; PO, oral; postmenopausal women; metabolism of ugt; Elderly → ;Hepatic cirrhosis, cirr ↓ ;RD, renal impairment, Renal disease，including uremia → ; The Pharmacological Basis of Therapeutics
Clearance 0.65 L/h/kg 10.8 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 2348.0 L/kg 2348.0 L/kg Oral single dose; postmenopausal women; DRUGBANK
Volume of Distribution 2853.0 L/kg 2853.0 L/kg Oral multiple dose; postmenopausal women; DRUGBANK
Volume of Distribution 2348.0 L/kg 2348±1220 L/kg Apparent volume of distribution; PO, oral; postmenopausal women; metabolism of ugt; The Pharmacological Basis of Therapeutics
Volume of Distribution 7.5 L/kg 7.5 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 29.5 h 27-32 h elimination half-life; DRUGBANK
Half-life 28.0 h 28(11-273) h postmenopausal women; The Pharmacological Basis of Therapeutics
Half-life 12.1 h 12.1 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity LD50 5000.0 mg/kg >5000 mg/kg PO, oral; Rattus, Rat; DRUGBANK
Eliminate Route 0.20 % <0.2 % Urinary excretion; Unchanged drug; DRUGBANK
Eliminate Route 0.20 % <0.2 % Urinary excretion; postmenopausal women; Unchanged drug; The Pharmacological Basis of Therapeutics
Protein Binding 95.0 % ~95 % plasma proteins; DRUGBANK
Protein Binding 95.0 % >95 % postmenopausal women; 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 adults 60.0 mg/day 60 mg/day PO, oral Evista raloxifene hydrochloride PDR
Max dose for elderly 60.0 mg/day 60 mg/day PO, oral Evista raloxifene hydrochloride 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