CASPOFUNGIN ACETATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C52H88N10O15.2C2H4O2
Molecular Weight	1213.417
Optical Activity	UNSPECIFIED
Defined Stereocenters	16 / 16
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(O)=O.CC(O)=O.CC[C@H](C)C[C@H](C)CCCCCCCCC(=O)N[C@H]1C[C@@H](O)[C@@H](NCCN)NC(=O)[C@@H]2[C@@H](O)CCN2C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]3C[C@@H](O)CN3C(=O)[C@@H](NC1=O)[C@@H](C)O)[C@H](O)[C@@H](O)C4=CC=C(O)C=C4)[C@H](O)CCN

InChI

InChIKey=OGUJBRYAAJYXQP-IJFZAWIJSA-N

InChI=1S/C52H88N10O15.2C2H4O2/c1-5-28(2)24-29(3)12-10-8-6-7-9-11-13-39(69)56-34-26-38(68)46(55-22-21-54)60-50(75)43-37(67)19-23-61(43)52(77)41(36(66)18-20-53)58-49(74)42(45(71)44(70)31-14-16-32(64)17-15-31)59-48(73)35-25-33(65)27-62(35)51(76)40(30(4)63)57-47(34)72;2*1-2(3)4/h14-17,28-30,33-38,40-46,55,63-68,70-71H,5-13,18-27,53-54H2,1-4H3,(H,56,69)(H,57,72)(H,58,74)(H,59,73)(H,60,75);2*1H3,(H,3,4)/t28-,29+,30+,33+,34-,35-,36+,37-,38+,40-,41-,42-,43-,44-,45-,46-;;/m0../s1

HIDE SMILES / InChI

Molecular Formula	C2H4O2
Molecular Weight	60.052
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C52H88N10O15
Molecular Weight	1093.3131
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	16 / 16
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021227s034s035lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/16162025

Caspofungin is an echinocandin antifungal drug, which is approved and is sold under the brand worldwide name cancidas. Caspofungin 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. Cancidas is indicated for the treatment of candidemia and the following candida infections: intra-abdominal abscesses, peritonitis, and pleural space infections in adult and pediatric patients. Also is indicated for the treatment of esophageal candidiasis in adult and pediatric patients and for the treatment of invasive aspergillosis in adult and pediatric patients, but has not been studied as initial therapy for invasive aspergillosis.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
1,3-beta-glucan synthase 10 Target ID: CHEMBL2364673 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16162025	Inhibitor 8504
1,3-beta-glucan synthase 10 Target ID: CHEMBL2364674 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16162025	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Intra-abdominal abscesses 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021227s034s035lbl.pdf	Curative	Approved 8583	CANCIDAS Approved Use CANCIDAS® is indicated in adults and pediatric patients (3 months and older) for: Empirical therapy for presumed fungal infections in febrile, neutropenic patients Treatment of candidemia and the following Candida infections: intra-abdominal abscesses, peritonitis and pleural space infections. CANCIDAS has not been studied in endocarditis, osteomyelitis, and meningitis due to Candida. Treatment of esophageal candidiasis [see Clinical Studies (14.3) Launch Date 2001
Peritonitis 22 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021227s034s035lbl.pdf	Curative	Approved 8583	CANCIDAS Approved Use CANCIDAS® is indicated in adults and pediatric patients (3 months and older) for: Empirical therapy for presumed fungal infections in febrile, neutropenic patients Treatment of candidemia and the following Candida infections: intra-abdominal abscesses, peritonitis and pleural space infections. CANCIDAS has not been studied in endocarditis, osteomyelitis, and meningitis due to Candida. Treatment of esophageal candidiasis [see Clinical Studies (14.3) Launch Date 2001
Candidemia 3 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021227s034s035lbl.pdf	Curative	Approved 8583	CANCIDAS Approved Use CANCIDAS® is indicated in adults and pediatric patients (3 months and older) for: Empirical therapy for presumed fungal infections in febrile, neutropenic patients Treatment of candidemia and the following Candida infections: intra-abdominal abscesses, peritonitis and pleural space infections. CANCIDAS has not been studied in endocarditis, osteomyelitis, and meningitis due to Candida. Treatment of esophageal candidiasis [see Clinical Studies (14.3) Launch Date 2001
Esophageal candidiasis 9 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021227s034s035lbl.pdf	Curative	Approved 8583	CANCIDAS Approved Use CANCIDAS® is indicated in adults and pediatric patients (3 months and older) for: Empirical therapy for presumed fungal infections in febrile, neutropenic patients Treatment of candidemia and the following Candida infections: intra-abdominal abscesses, peritonitis and pleural space infections. CANCIDAS has not been studied in endocarditis, osteomyelitis, and meningitis due to Candida. Treatment of esophageal candidiasis [see Clinical Studies (14.3) Launch Date 2001
Invasive aspergillosis 15 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021227s034s035lbl.pdf	Curative	Approved 8583	CANCIDAS Approved Use CANCIDAS® is indicated in adults and pediatric patients (3 months and older) for: Empirical therapy for presumed fungal infections in febrile, neutropenic patients Treatment of candidemia and the following Candida infections: intra-abdominal abscesses, peritonitis and pleural space infections. CANCIDAS has not been studied in endocarditis, osteomyelitis, and meningitis due to Candida. Treatment of esophageal candidiasis [see Clinical Studies (14.3) Launch Date 2001

C_max

Value	Dose	Co-administered	Analyte	Population
7.51 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25139840	50 mg 1 times / day multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		CASPOFUNGIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.65 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25139840	50 mg 1 times / day steady-state, intravenous dose: 50 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:		CASPOFUNGIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
88.7 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25139840	50 mg 1 times / day multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		CASPOFUNGIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
107.2 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25139840	50 mg 1 times / day steady-state, intravenous dose: 50 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:		CASPOFUNGIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
15.67 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25139840	50 mg 1 times / day multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:		CASPOFUNGIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
18.49 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25139840	50 mg 1 times / day steady-state, intravenous dose: 50 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:		CASPOFUNGIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
3% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021227s038lbl.pdf			CASPOFUNGIN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
113 mg 1 times / day multiple, intravenous Overdose Dose: 113 mg, 1 times / day Route: intravenous Route: multiple Dose: 113 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206110lbl.pdf	healthy, 16 years Health Status: healthy Age Group: 16 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206110lbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206110lbl.pdf
50 mg/m2 1 times / day multiple, intravenous Recommended Dose: 50 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 50 mg/m2, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19779392	unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sources: https://pubmed.ncbi.nlm.nih.gov/19779392	Disc. AE: Hypotension, Rash... AEs leading to discontinuation/dose reduction: Hypotension (1 patient) Rash (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/19779392
70 mg single, intravenous Dose: 70 mg Route: intravenous Route: single Dose: 70 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23761719	unhealthy, 58 years Health Status: unhealthy Age Group: 58 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/23761719	Other AEs: Kounis syndrome... Other AEs: Kounis syndrome (grade 5, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/23761719
70 mg single, intravenous Dose: 70 mg Route: intravenous Route: single Dose: 70 mg Sources: https://pubmed.ncbi.nlm.nih.gov/20407030	unhealthy, 86 years Health Status: unhealthy Age Group: 86 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/20407030	Disc. AE: Toxic epidermal necrolysis... AEs leading to discontinuation/dose reduction: Toxic epidermal necrolysis (severe, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/20407030
250 mg single, intravenous Highest studied dose Dose: 250 mg Route: intravenous Route: single Dose: 250 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206110lbl.pdf	healthy, adult Health Status: healthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206110lbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206110lbl.pdf

AEs

AE	Significance	Dose	Population
Hypotension	1 patient Disc. AE	50 mg/m2 1 times / day multiple, intravenous Recommended Dose: 50 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 50 mg/m2, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19779392	unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sources: https://pubmed.ncbi.nlm.nih.gov/19779392
Rash	1 patient Disc. AE	50 mg/m2 1 times / day multiple, intravenous Recommended Dose: 50 mg/m2, 1 times / day Route: intravenous Route: multiple Dose: 50 mg/m2, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19779392	unhealthy, 2-11 years Health Status: unhealthy Age Group: 2-11 years Sources: https://pubmed.ncbi.nlm.nih.gov/19779392
Kounis syndrome	grade 5, 1 patient	70 mg single, intravenous Dose: 70 mg Route: intravenous Route: single Dose: 70 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23761719	unhealthy, 58 years Health Status: unhealthy Age Group: 58 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/23761719
Toxic epidermal necrolysis	severe, 1 patient Disc. AE	70 mg single, intravenous Dose: 70 mg Route: intravenous Route: single Dose: 70 mg Sources: https://pubmed.ncbi.nlm.nih.gov/20407030	unhealthy, 86 years Health Status: unhealthy Age Group: 86 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/20407030

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252	inhibitor 2438	inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 OATP1B1 1079 NTCP 39 OCT1 620 OAT1 725 CYP1A2 2153 CYP2A6 879 CYP2C19 2057	P-gp 2052 OATP1B1 503 OATP1B3 435 CYP 303

Drug as perpetrator

Target	Modality	Activity	Metabolite
CYP2C19 2141	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=23 Page: (PMDA_I100) 23	likely [IC50 131 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=23 Page: (PMDA_I100) 23	likely [IC50 186 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=23 Page: (PMDA_I100) 23	likely [IC50 213 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=23 Page: (PMDA_I100) 23	likely [IC50 216 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=23 Page: (PMDA_I100) 23	likely [IC50 217 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=15 Page: (PMDA_I100) 15	no [IC50 >100 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=24 Page: (PMDA_I100) 24	no [IC50 >200 uM]	L-000747969 2
CYP2A6 911	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=24 Page: (PMDA_I100) 24	no [IC50 >200 uM]	L-000747969 2
CYP2C19 2141	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=24 Page: (PMDA_I100) 24	no [IC50 >200 uM]	L-000747969 2
CYP2C9 2497	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=24 Page: (PMDA_I100) 24	no [IC50 >200 uM]	L-000747969 2
CYP2D6 2546	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=24 Page: (PMDA_I100) 24	no [IC50 >200 uM]	L-000747969 2
CYP3A4 2633	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=24 Page: (PMDA_I100) 24	no [IC50 >200 uM]	L-000747969 2
OAT1 730	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=16 \| https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjQxMzQ3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ5OTgwOCJ9fQ%3D%3D Page: (PMDA_I100) 16	weak
OCT1 656	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=16 \| https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1Njg1IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ5OTgwOCJ9fQ%3D%3D Page: (PMDA_I100) 16	weak
NTCP 40	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=16 \| https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1Mjg3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNBU1BPRlVOR0lOIn19 Page: (PMDA_I100) 16	yes
OATP1B1 1095	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=16 \| https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjk3NjY4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ5OTgwOCJ9fQ%3D%3D Page: (PMDA_I100) 16	yes

Drug as victim

Target	Modality	Activity
OATP1B1 503	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=15 Page: (PMDA_I100) 15-16	likely
CYP 303	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=23 Page: (PMDA_I100) 23	no
OATP1B3 435	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=16 Page: (PMDA_I100) 16	no
P-gp 2052	substrate 4014 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=15 Page: (PMDA_I100) 15	no

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA001TCU	https://www.aablocks.com/goods/Goods/detail?id=AA001TCU
Acorn PharmaTech	ACN-036877	http://www.acornpharmatech.com/
Angel Pharmatech	AG308888	http://www.angelpharmatech.com/162808-62-0.html
AvaChem Scientific	3117B	http://www.avachem.com/productSearch.asp?3117B
BLD Pharm	BD120158	http://www.bldpharm.com/products/162808-62-0.html
ChemMol	49404681	http://www.chemmol.com/chemmol/49404681.html
eNovation Chemicals	D679169	https://www.enovationchem.com/ProductDetails.asp?ProductID=D679169
Finetech	FT-0696944	http://www.finetechnology-ind.com/prod/detail/pub/162808-62-0.html
iChemical	EBD53639	http://www.ichemical.com/chemicals/cas-162808-62-0
Lab Network	LN01344893	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01344893
MolPort	MolPort-044-559-990	https://www.molport.com/shop/molecule-link/MolPort-044-559-990
Parchem	28473	http://www.parchem.com/chemical-supplier-distributor/Caspofungin-018473.aspx
Smolecule	S570598	https://www.smolecule.com/products/s570598
THE BioTek	bt-242404	https://www.thebiotek.com/product/peptides/bt-242404

PubMed

Title	Date	PubMed
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.	2015-05-18	25811541
Recent advances in the treatment of mucormycosis.	2010-11	21308550
Evaluating retinal toxicity of intravitreal caspofungin in the mouse eye.	2010-11	20505203
Gateways to clinical trials.	2010-06	20664824
Echinocandins: A ray of hope in antifungal drug therapy.	2010-02	20606829
Treatment for multiple Aspergillus spondylitis including a hip joint.	2009-12	20404956
Gateways to clinical trials.	2009-11	20094643
Genomic analysis of the basal lineage fungus Rhizopus oryzae reveals a whole-genome duplication.	2009-07	19578406
Gateways to clinical trials.	2009-06	19649342
Gateways to Clinical Trials.	2008-11	19229381
Acute refractory hyperkalaemia and fatal cardiac arrest related to administration of liposomal amphotericin B.	2008-11	19011270
Gateways to clinical trials. July-August 2008.	2008-10-14	18850047
[Tolerance of caspofungin in intensive care unit: a prospective study].	2008-10	18835682
Gateways to clinical trials.	2008-09	18985183
Visual compatibility of caspofungin acetate with commonly used drugs during simulated Y-site delivery.	2008-03-01	18281738
Comedication of caspofungin acetate and cyclosporine A after allogeneic haematopoietic stem cell transplantation leads to negligible hepatotoxicity.	2008	18471157
Gateways to clinical trials.	2007-10	18040531
[A retrospective study of amphotericin B treatment for invasive fungal infection].	2007-09	18028796
Antimicrobial susceptibility of Fusarium, Aspergillus, and other filamentous fungi isolated from keratitis.	2007-06	17562990
Comparison of echinocandin antifungals.	2007-03	18360617
Comparison of antifungal treatments for murine fusariosis.	2006-11	16973654
Gateways to clinical trials.	2006-10	17136234
Gateways to clinical trials.	2006-09	17003851
Gateways to clinical trials.	2006-08-09	16894408
Limitations of caspofungin in the treatment of obstructive pyonephrosis due to Candida glabrata infection.	2006-08-08	16895593
FsFKS1, the 1,3-beta-glucan synthase from the caspofungin-resistant fungus Fusarium solani.	2006-07	16835448
Voriconazole in the management of nosocomial invasive fungal infections.	2006-06	18360588
Gateways to clinical trials.	2006-05	16801985
Gateways to clinical trials.	2006-03-17	16541195
Gateways to clinical trials.	2005-12	16395422
Gateways to clinical trials.	2005-11	16357953
Candida glabrata prosthetic valve endocarditis treated successfully with fluconazole plus caspofungin without surgery: a case report and literature review.	2005-11	16283214
Comparison of galactomannan detection, PCR-enzyme-linked immunosorbent assay, and real-time PCR for diagnosis of invasive aspergillosis in a neutropenic rat model and effect of caspofungin acetate.	2005-11	16275948
Gateways to clinical trials.	2005-10	16273137
Gateways to clinical trials.	2005-09-24	16179960
Caspofungin versus amphotericin B for candidemia: a pharmacoeconomic analysis.	2005-06	16117996
Gateways to clinical trials.	2005-06	16082422
Gateways to clinical trials.	2005-05	16082427
Fatal Blastoschizomyces capitatus sepsis in a neutropenic patient with acute myeloid leukemia: first documented case from Greece.	2005-05	15842341
Gateways to clinical trials.	2005-04-19	15834459
Gateways to clinical trials.	2005-03	15834466
Gateways to clinical trials.	2004-10	15605126
Caspofungin versus liposomal amphotericin B for empirical antifungal therapy in patients with persistent fever and neutropenia.	2004-09-30	15459300
Gateways to clinical trials.	2004-09-07	15349141
Gateways to clinical trials.	2004-06	15319815
Analysis of beta-1,3-glucan assembly in Saccharomyces cerevisiae using a synthetic interaction network and altered sensitivity to caspofungin.	2004-05	15166135
Gateways to clinical trials.	2004-03	15071612
Aspergillus nidulans RhoA is involved in polar growth, branching, and cell wall synthesis.	2004-01	14643255
An advanced double column-switching technique (LC-LC) for liquid chromatography/electrospray ionisation tandem mass spectrometry for fully automated analysis of caspofungin.	2004	15517540
Gateways to clinical trials.	2003-12	14735233

Patents

Sample Use Guides

In Vivo Use Guide

Administer CANCIDAS (caspofungin acetate) by slow intravenous (IV) infusion over approximately 1 hour. Do not administer CANCIDAS by IV bolus administration. Recommended Dosage in Adult Patients [18 years of age and older] The dosage and duration of CANCIDAS treatment for each indication are as follows: Empirical Therapy for Presumed Fungal Infections in Febrile Neutropenic Patients Administer a single 70-mg loading dose on Day 1, followed by 50 mg once daily thereafter. Duration of treatment should be based on the patient’s clinical response. Continue empirical therapy until resolution of neutropenia. In general, treat patients found to have a fungal infection for a minimum of 14 days after the last positive culture and continue treatment for at least 7 days after both neutropenia and clinical symptoms are resolved. If the 50-mg dose is well tolerated but does not provide an adequate clinical response, the daily dose can be increased to 70 mg. Candidemia and Other Candida Infections: administer a single 70-mg loading dose on Day 1, followed by 50 mg once daily thereafter. Duration of treatment should be dictated by the patient’s clinical and microbiological response. In general, continue antifungal therapy for at least 14 days after the last positive culture. Patients with neutropenia who remain persistently neutropenic may warrant a longer course of therapy pending resolution of the neutropenia. Esophageal Candidiasis: the dose is 50 mg once daily for 7 to 14 days after symptom resolution. A 70-mg loading dose has not been studied for this indication. Because of the risk of relapse of oropharyngeal candidiasis in patients with HIV infections, suppressive oral therapy could be considered. Invasive Aspergillosis: administer a single 70-mg loading dose on Day 1, followed by 50 mg once daily thereafter. Duration of treatment should be based upon the severity of the patient’s underlying disease, recovery from immunosuppression, and clinical response.

Route of Administration: Intravenous

In Vitro Use Guide

It was evaluated the susceptibility of 27 clinical isolates of Pythium insidiosum to caspofungin in vitro. Three reading criteria for MICs were adopted: MIC0, MIC1 and MIC2 (100%, 90% and 50% growth inhibition, respectively). Of the isolates 51.8% had an MIC0 of 64 mg/L, 88.8% of isolates had an MIC1 between 8 and 64 mg/L and 62.9% of isolates had a minimum fungicidal concentration of 64 mg/L. The results showed that caspofungin had limited fungistatic activity against P. insidiosum.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:20:36 GMT 2025` Edited by `admin` on `Mon Mar 31 18:20:36 GMT 2025`
Record UNII	VUW370O5QE
Record Status	`Validated (UNII)`
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Name

Type

Language

CASPOFUNGIN ACETATE [USAN]

Preferred Name

English

CASPOFUNGIN ACETATE

Official Name

English

CASPOFUNGIN ACETATE [VANDF]

Common Name

English

CANCIDAS

Brand Name

English

CASPOFUNGIN ACETATE [MART.]

Common Name

English

Caspofungin acetate [WHO-DD]

Common Name

English

1-((4R,5S)-5-((2-AMINOETHYL)AMINO)-N(SUP 2)-(10,12-DIMETHYL-1-OXOTETRADECYL)-4-HYDROXY-L-ORNITHINE)-5-((3R)-3-HYDROXY-L-ORNITHINE)PNEUMOCANDIN B(SUB 0), DIACETATE (SALT)

Common Name

English

MK-0991

Code

English

CASPOFUNGIN DIACETATE

Common Name

English

CASPOFUNGIN ACETATE [MI]

Common Name

English

CASPOFUNGIN ACETATE [JAN]

Common Name

English

CASPOFUNGIN ACETATE [ORANGE BOOK]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C514