Molecular Formula	Cl2H4N2Pt
Molecular Weight	298
Structure
State	solid
Clearance	* 15-16 L/h/m^2 [total body clearance, 7-hour infusion of 100 mg/m^2] * 62 mL/min/m^2 [renal clearance, 2-hour infusion of 100 mg/m^2] * 50 mL/min/m^2 [renal clearance, 6- to 7-hour infusion of 100 mg/m^2] The renal clearance of free (ultrafilterable) platinum also exceeds the glomerular filtration rate indicating that cisplatin or other platinum-containing molecules are actively secreted by the kidneys. The renal clearance of free platinum is nonlinear and variable and is dependent on dose, urine flow rate, and individual variability in the extent of active secretion and possible tubular reabsorption.
Volume of distribution	Volume of distribution at steady state = 11-12 L/m^2
Route of elimination	The parent compound, cisplatin, is excreted in the urine. Although small amounts of platinum are present in the bile and large intestine after administration of cisplatin, the fecal excretion of platinum appears to be insignificant.
Protein binding	Cisplatin does not undergo instantaneous and reversible binding to plasma protein that is characteristic of normal drug-protein binding. However, the platinum itself is capable of binding to plasma proteins, including albumin, transferrin, and gamma globulin. Three hours after a bolus injection and two hours after the end of a three-hour infusion, 90% of the plasma platinum is protein bound.
Half life	Cisplatin decays monoexponentially with a half life of 20 to 30 minutes following administrations of 50 or 100 mg/m^2. Cisplatin has a plasma half-life of 30 minutes. The complexes between albumin and the platinum from cisplatin do not dissociate to a significant extent and are slowly eliminated with a minimum half-life of five days or more.
Absorption	Following cisplatin doses of 20 to 120 mg/m^2, the concentrations of platinum are highest in liver, prostate, and kidney; somewhat lower in bladder, muscle, testicle, pancreas, and spleen; and lowest in bowel, adrenal, heart, lung, cerebrum, and cerebellum. Platinum is present in tissues for as long as 180 days after the last administration.
Trade names	Platinol
Description	Anticaner; platinum-based chemotherapy drug

Toxicity	Dose	Time	Species	Model	Method	Action	Positive criterion	Reference
TRANSMEMBRANE POTENTIAL		1 or 3 hr		Ishikawa and Caco-2	JC-10 fluorescent dye	decrease		299
PERMEABILIZATION				U2OS	release of Smac m cherry(IMS-RP probe is a non-functional variant of mitochondrial protein Smac - mCherry fusion protein that acts as an indicator of mitochondrial permeabilization in live cells)	induce		313
ATP TURNOVER						decrease		307
GLUCOSE GALACTOSE IC50 RATIO	1			LUHMES (Lund human mesencephalic) cells	Glc–Gal–NeuriTox assay	Negative	EC25(NA) [Glc/Gal]	326
SHAPE								197
MITOCHONDRIAL DYNAMICS	3 mg/kg bodyweight	twice a week for 2 weeks	Mouse	Mouse tibial nerves and dorsal root ganglia (L1–L4)				247
ROS PRODUCTION	84.96 ± 3, 158.9 ± 8.2, 372.7 ± 17.5 and 499.5 ± 15.1 μM	24 hr		Ishikawa, MDA-MB-231, PC-3 and Caco-2	Intracellular ROS (a) and mitochondrial superoxide were measured by fluorescence intensity of H2DCFDA and MitoSOX respectively.	increase	IC50	299
ROS PRODUCTION	150 µM	24hr		U2OS	U2OS cells stably expressing mt-roGFP and HyPer-red targeted at mitochondria	increase		313
ROS PRODUCTION						Increase		307
MITOCHONDRIAL DNA METABOLIC PROCESS		24 hr		Caco-2 and Ishikawa cells	Relative quantification of mtDNA copy number was measured using the QuantiTect SYBR Green PCR kit	decrease		299
MITOCHONDRIAL DNA DAMAGE						Increase		307
APOPTOSIS		24 hr		Ishikawa and Caco-2	WB was performed to measure the BCL-XL and released cytochrome c proteins from mitochondria; Caspase-3/7 activity was measured using the Caspase-Glo 3/7 reagent from the ApoTox-Glo Triplex Assay kit	induce		299

Target	Dose	Time	Species	Model	Method	Action	Positive criterion	Reference
Reactive oxygen species						increase		307

Organism	Test type	Route	Dose (normalized dose)	Effect	Source
guinea pig	LD50	intraperitoneal	9700ug/kg (9.7mg/kg)	sense organs and special senses: change in acuity: ear	Toxicology and Applied Pharmacology. Vol. 33, Pg. 320, 1975.
dog	LDLo	intravenous	2500ug/kg (2.5mg/kg)		Toxicology and Applied Pharmacology. Vol. 25, Pg. 230, 1973.
mouse	LD50	intramuscular	17900ug/kg (17.9mg/kg)		Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 10, Pg. 723, 1982.
human	TDLo	intravenous	1500ug/kg/6D- (1.5mg/kg)		Cancer Chemotherapy Reports, Part 1. Vol. 57, Pg. 191, 1973.
human	TDLo	intravenous	500ug/kg/13D- (0.5mg/kg)		Cancer Treatment Reports. Vol. 62, Pg. 693, 1978.
rat	LD	unreported	> 5mg/kg (5mg/kg)	kidney, ureter, and bladder: "changes in tubules (including acute renal failure, acute tubular necrosis)"	Journal of Toxicological Sciences. Vol. 24, Pg. 337, 1999.
human	TDLo	intravenous	72mg/kg/25D-I (72mg/kg)	gastrointestinal: nausea or vomiting	Cancer Treatment Reports. Vol. 62, Pg. 1591, 1978.
mammal (species unspecified)	LDLo	intravenous	8mg/kg (8mg/kg)	gastrointestinal: nausea or vomiting	Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 28(4), Pg. 285, 2000.
mouse	LD50	intravenous	11mg/kg (11mg/kg)		Archives of Toxicology, Supplement. Vol. 7, Pg. 90, 1984.
mouse	LD50	parenteral	22mg/kg (22mg/kg)		International Journal of Radiation Oncology, Biology, Physics. Vol. 5, Pg. 1417, 1979.
rat	LD50	oral	25800ug/kg (25.8mg/kg)		Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 10, Pg. 723, 1982.
man	TDLo	parenteral	2140ug/kg/5D- (2.14mg/kg)	kidney, ureter, and bladder: "changes in tubules (including acute renal failure, acute tubular necrosis)"	Nippon Naika Gakkai Zasshi. Journal of the Japanese Society of Internal Medicine. Vol. 72, Pg. 1426, 1983.
mouse	LD50	intraperitoneal	6600ug/kg (6.6mg/kg)		Journal of Medicinal Chemistry. Vol. 34, Pg. 414, 1991.
rat	LD50	intramuscular	9200ug/kg (9.2mg/kg)		Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 10, Pg. 723, 1982.
human	TDLo	intravenous	2500ug/kg (2.5mg/kg)		Cancer Chemotherapy Reports, Part 1. Vol. 59, Pg. 647, 1975.
mouse	LD50	subcutaneous	13mg/kg (13mg/kg)		Journal de Pharmacie de Belgique. Vol. 41, Pg. 286, 1986.
mouse	LD50	unreported	10900ug/kg (10.9mg/kg)		Gan to Kagaku Ryoho. Cancer and Chemotherapy. Vol. 13, Pg. 280, 1986.
rat	LD50	intraperitoneal	6400ug/kg (6.4mg/kg)		Journal of Toxicological Sciences. Vol. 18, Pg. 31, 1993.
child	TDLo	unreported	19200ug/kg/12 (19.2mg/kg)	sense organs and special senses: change in acuity: ear	Journal of Pediatrics. Vol. 103, Pg. 1006, 1983.
frog	LD50	parenteral	17mg/kg (17mg/kg)		Journal of Comparative Pathology. Vol. 103, Pg. 387, 1990.
mouse	LD50	oral	32700ug/kg (32.7mg/kg)		Kiso to Rinsho. Clinical Report. Vol. 15, Pg. 5669, 1981.
monkey	LDLo	intravenous	250ug/kg (0.25mg/kg)		Cancer Vol. 33, Pg. 1219, 1974.
human	TDLo	intradermal	40ng/kg (0.00004mg/kg)		Cancer Research. Vol. 35, Pg. 2766, 1975.
man	TDLo	intravenous	2140ug/kg/5D- (2.14mg/kg)	kidney, ureter, and bladder: "changes in tubules (including acute renal failure, acute tubular necrosis)"	Japanese Journal of Medicine. Vol. 23, Pg. 283, 1984.
rat	LD50	subcutaneous	8100ug/kg (8.1mg/kg)		Kiso to Rinsho. Clinical Report. Vol. 15, Pg. 5669, 1981.
mouse	LD50	intraperitoneal	27mg/kg (27mg/kg)		Chemico-Biological Interactions. Vol. 5, Pg. 415, 1972.
rat	LD50	intravenous	8mg/kg (8mg/kg)	kidney, ureter, and bladder: other changes	JNCI, Journal of the National Cancer Institute. Vol. 67, Pg. 201, 1981.

Adrenal gland cancer

Anal cancer

Bladder transitional cell carcinoma

Brain neoplasm malignant

Breast cancer

Cervix carcinoma

Choriocarcinoma

Endometrial cancer

Gestational trophoblastic tumour

Hepatic cancer

Hodgkin's disease

Hodgkin's disease lymphocyte depletion type stage unspecified

Hodgkin's disease lymphocyte predominance type stage unspecified

Hypocalcaemia

Hypomagnesaemia

Lung neoplasm malignant

Lymphoma

Malignant melanoma

Mesothelioma

Neoplasm

Neutropenia

Non-Hodgkin's lymphoma

Oesophageal carcinoma

Osteosarcoma

Ovarian neoplasm

Penile cancer

Prostate cancer

Renal cancer

Renal failure

Renal impairment

Sarcoma

Squamous cell carcinoma

Testicular neoplasm

Ototoxicity (0.31)

Tinnitus (0.09)

AB00642613-02	AB00642613_03	AC-2109
AKOS025401526	BCP9000536	BDBM50028111
BRD-K69172251-001-01-4	CAS-15663-27-1	CS-1122
Cisplatin(cis-Diammenedichloroplatinum)	DB00515	DSSTox_CID_4983
DSSTox_GSID_24983	DSSTox_RID_77611	DTXSID4024983
FT-0082333	FT-0623946	HMS3268F06
HMS3654E14	HY-17394	NCGC00090759-01
NCGC00090759-02	NCGC00090759-03	NCGC00260049-01
NCGC00263537-01	NSC-131558	NSC-241517
NSC131558	NSC241517	Neuro_000055
Platinum (II) complex	Platinum(IV) Complex	Platinum, diamminedichloro-
Pt(II) Complex	Replaced CAS registry number(s): 14283-03-5	SW222225-1
Tox21_111011	Tox21_111011_1	Tox21_113470
Tox21_202500	camphorato platinum complex derivative	cis-Diaminedichloroplatinum
cis-Diammine-dichloroplatinum(II)	cis-Diamminedichlorplatine	cis-Dichlorodiamine platinum
cis-Platinum diamminedichloride	cis-Platinum(II)	cis-diamminedichloroplatinum(II)(cis-DDP)
cisplatin complex	dichloromethanediamine(platinum complex)	dichloroplatinumdiamine
trans-Diaminedichloroplatinum	trans-dichlorodiammineplatinum.(transplatin)

DrugBank Name	Cisplatin
DrugBank	DB00515
CAS Number	14913-33-8, 15663-27-1, 26035-31-4
PubChem Compound	2767
KEGG Compound ID	C06911
KEGG Drug	D00275
PubChem.Substance	46504561
ChEBI	27899
PharmGKB	PA449014
ChemSpider	76401
BindingDB	50028111.0
TTD	DAP000215
Wikipedia	Cisplatin
HET	CPT
DPD	13121