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Details

Stereochemistry ACHIRAL
Molecular Formula C2H2O3.Pt.2H3N
Molecular Weight 303.181
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of NEDAPLATIN

SMILES

N.N.[Pt++].[O-]CC([O-])=O

InChI

InChIKey=GYAVMUDJCHAASE-UHFFFAOYSA-M
InChI=1S/C2H3O3.2H3N.Pt/c3-1-2(4)5;;;/h1H2,(H,4,5);2*1H3;/q-1;;;+2/p-1

HIDE SMILES / InChI

Molecular Formula H3N
Molecular Weight 17.0305
Charge 0
Count
MOL RATIO 2 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula Pt
Molecular Weight 195.084
Charge 2
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C2H2O3
Molecular Weight 74.0355
Charge -2
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Nedaplatin is a second-generation cisplatin analogue with antineoplastic activity. nedaplatin forms reactive platinum complexes that bind to nucelophillic groups in DNA, resulting in intrastrand and interstrand DNA cross-links, apoptosis and cell death. It is currently registered for the treatment of various cancers (head and neck, testicular, lung, ovarian, cervical, non-small-cell lung) in Japan. The most commonly reported adverse reactions include nausea, vomiting, loss of appetite and hair loss. Nedaplatin may also cause nephrotoxicity at therapeutic doses, especially in patients with deteriorating renal function.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
AQUPLA
Primary
AQUPLA
Primary
AQUPLA
Primary
AQUPLA
Primary
AQUPLA
Primary
AQUPLA
Primary
AQUPLA
Primary
AQUPLA

Cmax

ValueDoseCo-administeredAnalytePopulation
6.1 μg/mL
80 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens
6.34 μg/mL
100 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens
1.01 μg/mL
20 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
19.45 μg × h/mL
80 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens
30 μg × h/mL
100 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens
2.59 μg × h/mL
20 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
5.69 h
80 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens
5.3 h
100 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens
2.1 h
20 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
19%
100 mg/m² single, intravenous
PLATINUM plasma
Homo sapiens

Doses

AEs

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
Once daily over 60 minutes or longer, and then it is discontinued for at least 4 weeks. This dosing schedule as 1 course is repeated.
Route of Administration: Intravenous
In Vitro Use Guide
Nedaplatin inhibited the proliferation of SBC-3 cells by 98%, 93%, 75%, 54%, 27%, 6%, and 2% at a concentration of 0.005, 0.01, 0.025, 0.05, 0.1, 0.25, and 0.5 ug/ml, respectively. Consequently, its IC50 value for growth inhibition of SBC-3 cells was 0.053 ug/ml.
Substance Class Chemical
Record UNII
8UQ3W6JXAN
Record Status Validated (UNII)
Record Version