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

Stem definition	Drug id	CAS RN
antifungal antibiotics	2977	162808-62-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: caspofungin acetate caspofungin diacetate cancidas caspofungin MK-0991	Caspofungin, an echinocandin, inhibits the synthesis of beta (1,3)-D-glucan, an essential component of the cell wall of susceptible Aspergillus species and Candida species. Beta (1,3)-D-glucan is not present in mammalian cells. Caspofungin has shown activity against Candida species and in regions of active cell growth of the hyphae of Aspergillus fumigatus. Molecular weight: 1093.33 Formula: C52H88N10O15 CLOGP: -2.35 LIPINSKI: 3 HAC: 25 HDO: 16 TPSA: 412.03 ALOGS: -3.47 ROTB: 23 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

caspofungin acetate
caspofungin diacetate
cancidas
caspofungin
MK-0991

Caspofungin, an echinocandin, inhibits the synthesis of beta (1,3)-D-glucan, an essential component of the cell wall of susceptible Aspergillus species and Candida species. Beta (1,3)-D-glucan is not present in mammalian cells. Caspofungin has shown activity against Candida species and in regions of active cell growth of the hyphae of Aspergillus fumigatus.

Molecular weight: 1093.33
Formula: C52H88N10O15
CLOGP: -2.35
LIPINSKI: 3
HAC: 25
HDO: 16
TPSA: 412.03
ALOGS: -3.47
ROTB: 23

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
50	mg	P

ADMET properties:

Show entries

Search:

Property	Value	Reference
t_half (Half-life)	27 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	15 mg/mL	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	1.40 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.91 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	0.14 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.13 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.04 %	Lombardo F, Berellini G, Obach RS

Showing 1 to 8 of 8 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
Jan. 26, 2001	FDA	MERCK

FDA Adverse Event Reporting System (Female)

Show entries

Search:

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
Systemic mycosis	256.85	27.97	53	8123	1144	63479702
Septic shock	230.11	27.97	129	8047	66500	63414346
Multiple organ dysfunction syndrome	226.72	27.97	121	8055	56631	63424215
Bronchopulmonary aspergillosis	176.63	27.97	59	8117	8576	63472270
Upper respiratory fungal infection	164.00	27.97	27	8149	151	63480695
Drug resistance	145.36	27.97	67	8109	22866	63457980
Drug ineffective	136.13	27.97	364	7812	1044401	62436445
Mucormycosis	129.27	27.97	36	8140	2835	63478011
Aspergillus infection	125.60	27.97	45	8131	8048	63472798
Diffuse large B-cell lymphoma refractory	122.30	27.97	29	8147	1201	63479645

Showing 1 to 10 of 93 entries

Previous1 2 3 4 5…10Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

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
Drug ineffective	326.13	22.54	537	10345	456214	34489835
Multiple organ dysfunction syndrome	212.97	22.54	182	10700	76384	34869665
Aspergillus infection	208.20	22.54	93	10789	12161	34933888
Systemic mycosis	205.30	22.54	55	10827	1518	34944531
Drug resistance	201.79	22.54	116	10766	25811	34920238
Bronchopulmonary aspergillosis	153.94	22.54	80	10802	14579	34931470
Septic shock	139.80	22.54	140	10742	71694	34874355
Pathogen resistance	139.11	22.54	65	10817	9417	34936632
Dysplastic naevus	138.89	22.54	32	10850	464	34945585
Solar lentigo	135.65	22.54	32	10850	517	34945532

Showing 1 to 10 of 91 entries

Previous1 2 3 4 5…10Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

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
Drug ineffective	495.60	22.72	877	17257	1080036	78646218
Systemic mycosis	447.46	22.72	107	18027	2559	79723695
Multiple organ dysfunction syndrome	384.18	22.72	273	17861	119973	79606281
Bronchopulmonary aspergillosis	336.81	22.72	142	17992	22152	79704102
Aspergillus infection	316.23	22.72	130	18004	19031	79707223
Septic shock	301.12	22.72	238	17896	122563	79603691
Pathogen resistance	205.44	22.72	88	18046	14254	79712000
Drug resistance	195.57	22.72	121	18013	42092	79684162
Mucormycosis	169.30	22.72	66	18068	8403	79717851
Drug reaction with eosinophilia and systemic symptoms	169.14	22.72	130	18004	64114	79662140

Showing 1 to 10 of 164 entries

Previous1 2 3 4 5…17Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	J02AX04	ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE Other antimycotics for systemic use
CHEBI has role	CHEBI:35441	antiinfective agents
FDA CS	M0519359	Lipopeptides
FDA EPC	N0000175507	Echinocandin Antifungal
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000935	Antifungal Agents
MeSH PA	D004791	Enzyme Inhibitors

Showing 1 to 7 of 7 entries

Previous1Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Candidiasis of the esophagus	indication	20639004	DOID:13146
Candidemia	indication	432261003
Intra-Abdominal Candida Abscess	indication
Candida Pleural Space Infection	indication
Refractory Aspergillosis	indication
Candida Peritonitis	indication
Oropharyngeal Candidiasis	off-label use
Hypokalemia	contraindication	43339004
Liver function tests abnormal	contraindication	166603001
Disease of liver	contraindication	235856003	DOID:409

Showing 1 to 10 of 10 entries

Previous1Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Show entries

Search:

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.55	acidic
pKa2	11.98	acidic
pKa3	13.1	acidic
pKa4	13.77	acidic
pKa5	13.84	acidic
pKa6	10.04	Basic
pKa7	9.05	Basic
pKa8	4.09	Basic

Showing 1 to 8 of 8 entries

Previous1Next

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.22	CHEMBL
Beta-1,3-glucan synthase catalytic subunit 1	Enzyme		O13428_CANAX	INHIBITOR	IC50	8.89	WOMBAT-PK	CHEMBL
1,3-beta-glucan synthase catalytic subunit FksP	Enzyme		Q4WLT4_ASPFU	INHIBITOR			CHEMBL	CHEMBL
1,3-beta-D-glucan synthase catalytic subunit	Unclassified		O13383_CANAX		IC50	9.62	CHEMBL

Showing 1 to 4 of 4 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
009069	NDDF
009070	NDDF
129474002	SNOMEDCT_US
140108	RXNORM
15896	MMSL
16119814	PUBCHEM_CID
179463-17-3	SECONDARY_CAS_RN
260563	MMSL
4021253	VANDF
4021254	VUID

Showing 1 to 10 of 25 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
CANCIDAS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3822	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	5 mg	INTRAVENOUS	NDA	28 sections
CANCIDAS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3822	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	5 mg	INTRAVENOUS	NDA	28 sections
CANCIDAS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3823	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	7 mg	INTRAVENOUS	NDA	28 sections
CANCIDAS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3823	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	7 mg	INTRAVENOUS	NDA	28 sections
CASPOFUNGIN ACETATE	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3421	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	5 mg	INTRAVENOUS	ANDA	27 sections
CASPOFUNGIN ACETATE	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3423	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	7 mg	INTRAVENOUS	ANDA	27 sections
Caspofungin Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	25021-194	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	5 mg	INTRAVENOUS	ANDA	31 sections
Caspofungin Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	25021-195	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	7 mg	INTRAVENOUS	ANDA	31 sections
Caspofungin Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	63323-356	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	5 mg	INTRAVENOUS	NDA	29 sections
Caspofungin Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	63323-358	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	7 mg	INTRAVENOUS	NDA	29 sections

Showing 1 to 10 of 28 entries

Previous1 2 3Next