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cisplatin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antineoplastic agents, platinum derivatives	4392	15663-27-1

Description:

Molecule	Description
Synonyms: cisplatin platinum diamminodichloride cis-Platinum	An inorganic and water-soluble platinum complex. After undergoing hydrolysis, it reacts with DNA to produce both intra and interstrand crosslinks. These crosslinks appear to impair replication and transcription of DNA. The cytotoxicity of cisplatin correlates with cellular arrest in the G2 phase of the cell cycle. Molecular weight: 300.05 Formula: Cl2H6N2Pt CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

cisplatin
platinum diamminodichloride
cis-Platinum

An inorganic and water-soluble platinum complex. After undergoing hydrolysis, it reacts with DNA to produce both intra and interstrand crosslinks. These crosslinks appear to impair replication and transcription of DNA. The cytotoxicity of cisplatin correlates with cellular arrest in the G2 phase of the cell cycle.

Molecular weight: 300.05
Formula: Cl2H6N2Pt
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	4.75 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	2.53 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	2.30 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 19, 1978	FDA	HQ SPCLT PHARMA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	1196.26	15.18	945	58515	117504	63312058
Neutropenia	1169.36	15.18	1102	58358	173903	63255659
Disease progression	1092.92	15.18	910	58550	121848	63307714
Thrombocytopenia	833.89	15.18	858	58602	150299	63279263
Malignant neoplasm progression	676.97	15.18	583	58877	81538	63348024
Haematotoxicity	573.12	15.18	243	59217	9133	63420429
Mucosal inflammation	552.89	15.18	411	59049	46517	63383045
Bone marrow failure	539.09	15.18	338	59122	28952	63400610
Anaemia	474.86	15.18	924	58536	292506	63137056
Ototoxicity	426.69	15.18	120	59340	1242	63428320

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	1417.99	13.27	1713	84514	135136	34735568
Neutropenia	1019.04	13.27	1566	84661	155212	34715492
Disease progression	848.28	13.27	1181	85046	106896	34763808
Mucosal inflammation	763.61	13.27	685	85542	37937	34832767
Malignant neoplasm progression	602.26	13.27	902	85325	87144	34783560
Thrombocytopenia	602.23	13.27	1243	84984	155004	34715700
Myelosuppression	462.36	13.27	382	85845	18883	34851821
Pancytopenia	429.95	13.27	810	85417	94347	34776357
Bone marrow failure	376.86	13.27	411	85816	28842	34841862
Dehydration	351.56	13.27	900	85327	129069	34741635

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	2362.74	12.74	2333	124465	228666	79388924
Neutropenia	1941.01	12.74	2334	124464	285376	79332214
Disease progression	1406.73	12.74	1595	125203	182767	79434823
Thrombocytopenia	1369.03	12.74	1886	124912	263373	79354217
Malignant neoplasm progression	1256.39	12.74	1302	125496	134688	79482902
Mucosal inflammation	1155.74	12.74	959	125839	74621	79542969
Pancytopenia	898.26	12.74	1208	125590	164537	79453053
Bone marrow failure	836.65	12.74	675	126123	50432	79567158
Myelosuppression	834.37	12.74	612	126186	39684	79577906
Haematotoxicity	781.59	12.74	415	126383	15104	79602486

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XA01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Platinum compounds
CHEBI has role	CHEBI:25435	mutagens
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:47868	photosensitising agent
CHEBI has role	CHEBI:50684	cross-linking reagents
CHEBI has role	CHEBI:50902	genotoxic agent
CHEBI has role	CHEBI:61015	nephrotoxins
CHEBI has role	CHEBI:68495	Type I cell-death inducers
CHEBI has role	CHEBI:173085	ferroptosis inducers
FDA EPC	N0000175413	Platinum-based Drug

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Malignant tumor of ovary	indication	363443007	DOID:2394
Ovarian Germ Cell Tumor Carcinoma	indication
Testicular Germ Cell Tumor	indication
Invasive Bladder Malignancy	indication

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	Ki	5.95	CHEMBL
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN	Ki	5.37	CHEMBL
Canalicular multispecific organic anion transporter 1	Transporter	Q92887	MRP2_HUMAN			WOMBAT-PK
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN	Ki	5.62	DRUG MATRIX
Multidrug resistance-associated protein 6	Transporter	O95255	MRP6_HUMAN			WOMBAT-PK
Multidrug resistance-associated protein 5	Transporter	O15440	MRP5_HUMAN			WOMBAT-PK
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN	IC50	5.58	DRUG MATRIX
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN	IC50	4.64	DRUG MATRIX
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN	IC50	5.32	DRUG MATRIX
C-X-C chemokine receptor type 2	GPCR	P25025	CXCR2_HUMAN	Ki	5.02	DRUG MATRIX

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External reference:

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ID	Source
CPT	PDB_CHEM_ID
002641	NDDF
2555	RXNORM
31747	MMSL
387318005	SNOMEDCT_US
4018139	VUID
4018139	VANDF
4426	INN_ID
4456	MMSL
5343	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
CISplatin	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9504	INJECTION	1 mg	INTRAVENOUS	ANDA	19 sections
CISplatin	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9505	INJECTION	1 mg	INTRAVENOUS	ANDA	19 sections
Cisplatin	HUMAN PRESCRIPTION DRUG LABEL	1	0703-5747	INJECTION, SOLUTION	50 mg	INTRAVENOUS	ANDA	29 sections
Cisplatin	HUMAN PRESCRIPTION DRUG LABEL	1	0703-5747	INJECTION, SOLUTION	50 mg	INTRAVENOUS	ANDA	29 sections
Cisplatin	HUMAN PRESCRIPTION DRUG LABEL	1	0703-5748	INJECTION, SOLUTION	100 mg	INTRAVENOUS	ANDA	29 sections
Cisplatin	HUMAN PRESCRIPTION DRUG LABEL	1	0703-5748	INJECTION, SOLUTION	100 mg	INTRAVENOUS	ANDA	29 sections
Cisplatin	HUMAN PRESCRIPTION DRUG LABEL	1	16729-288	INJECTION	1 mg	INTRAVENOUS	ANDA	26 sections
Cisplatin	HUMAN PRESCRIPTION DRUG LABEL	1	25021-253	INJECTION, SOLUTION	1 mg	INTRAVENOUS	ANDA	21 sections
CISplatin	HUMAN PRESCRIPTION DRUG LABEL	1	44567-509	INJECTION, SOLUTION	1 mg	INTRAVENOUS	NDA	19 sections
CISplatin	HUMAN PRESCRIPTION DRUG LABEL	1	44567-510	INJECTION, SOLUTION	1 mg	INTRAVENOUS	NDA	19 sections

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