CASPOFUNGIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C52H88N10O15
Molecular Weight	1093.3131
Optical Activity	UNSPECIFIED
Defined Stereocenters	16 / 16
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12C[C@@H](O)CN1C(=O)[C@@]([H])(NC(=O)[C@H](C[C@@H](O)[C@@H](NCCN)NC(=O)[C@]3([H])[C@@H](O)CCN3C(=O)[C@@]([H])(NC(=O)[C@@]([H])(NC2=O)[C@H](O)[C@@H](O)C4=CC=C(O)C=C4)[C@H](O)CCN)NC(=O)CCCCCCCC[C@@H](C)C[C@@H](C)CC)[C@@H](C)O

InChI

InChIKey=JYIKNQVWKBUSNH-WVDDFWQHSA-N

InChI=1S/C52H88N10O15/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/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)/t28-,29+,30+,33+,34-,35-,36+,37-,38+,40-,41-,42-,43-,44-,45-,46-/m0/s1

HIDE SMILES / InChI

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 7 Target ID: CHEMBL2364673 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16162025	Inhibitor 8297
1,3-beta-glucan synthase 7 Target ID: CHEMBL2364674 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16162025	Inhibitor 8297

Conditions

Condition	Modality	Highest Phase	Product
Intra-abdominal abscesses 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021227s034s035lbl.pdf	Curative	Approved 8429	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 8429	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 8429	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 8429	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 14 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021227s034s035lbl.pdf	Curative	Approved 8429	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
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
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

AUC

Value	Dose	Co-administered	Analyte	Population
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
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

T_1/2

Value	Dose	Co-administered	Analyte	Population
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
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

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 (starting) 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 n = 1 Health Status: healthy Age Group: 16 years Population Size: 1 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 (starting) 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 n = 171 Health Status: unhealthy Age Group: 2-11 years Population Size: 171 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 (starting) Dose: 70 mg Route: intravenous Route: single Dose: 70 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23761719	unhealthy, 58 years n = 1 Health Status: unhealthy Age Group: 58 years Sex: M Population Size: 1 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 (starting) Dose: 70 mg Route: intravenous Route: single Dose: 70 mg Sources: https://pubmed.ncbi.nlm.nih.gov/20407030	unhealthy, 86 years n = 1 Health Status: unhealthy Age Group: 86 years Sex: M Population Size: 1 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 n = 6 Health Status: healthy Age Group: adult Population Size: 6 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 (starting) 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 n = 171 Health Status: unhealthy Age Group: 2-11 years Population Size: 171 Sources: https://pubmed.ncbi.nlm.nih.gov/19779392
Rash	1 patient Disc. AE	50 mg/m2 1 times / day multiple, intravenous (starting) 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 n = 171 Health Status: unhealthy Age Group: 2-11 years Population Size: 171 Sources: https://pubmed.ncbi.nlm.nih.gov/19779392
Kounis syndrome	grade 5, 1 patient	70 mg single, intravenous (starting) Dose: 70 mg Route: intravenous Route: single Dose: 70 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23761719	unhealthy, 58 years n = 1 Health Status: unhealthy Age Group: 58 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/23761719
Toxic epidermal necrolysis	severe, 1 patient Disc. AE	70 mg single, intravenous (starting) Dose: 70 mg Route: intravenous Route: single Dose: 70 mg Sources: https://pubmed.ncbi.nlm.nih.gov/20407030	unhealthy, 86 years n = 1 Health Status: unhealthy Age Group: 86 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/20407030

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 1587	inhibitor 1767	inhibitor 1852

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1461 OATP1B1 788 NTCP 34 OCT1 512 OAT1 599 CYP1A2 1524 CYP2A6 707 CYP2C19 1478	P-gp 1537 OATP1B1 406 OATP1B3 350 CYP 270

Drug as perpetrator

Target	Modality	Activity	Metabolite
CYP2C19 1553	inhibitor 3277 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 1692	inhibitor 3277 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 739	inhibitor 3277 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 1891	inhibitor 3277 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 1819	inhibitor 3277 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 1650	inhibitor 3277 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 1692	inhibitor 3277 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 739	inhibitor 3277 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 1553	inhibitor 3277 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 1819	inhibitor 3277 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 1891	inhibitor 3277 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 1925	inhibitor 3277 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 603	inhibitor 3277 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 543	inhibitor 3277 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 35	inhibitor 3277 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 803	inhibitor 3277 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 406	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=15 Page: (PMDA_I100) 15-16	likely
CYP 270	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=23 Page: (PMDA_I100) 23	no
OATP1B3 350	substrate 3367 Sources: https://www.pmda.go.jp/drugs/2012/P201200014/170050000_22400AMX00036_I100_1.pdf#page=16 Page: (PMDA_I100) 16	no
P-gp 1537	substrate 3367 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
Finetech	FT-0696944	http://www.finetechnology-ind.com/prod/detail/pub/162808-62-0.html
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
eNovation Chemicals	D679169	https://www.enovationchem.com/ProductDetails.asp?ProductID=D679169
iChemical	EBD53639	http://www.ichemical.com/chemicals/cas-162808-62-0

PubMed

Title	Date	PubMed
Caspofungin acetate: an antifungal agent.	2001 Jul 1	11449878
Caspofungin acetate, bivalirudin.	2001 Oct 1	11596694
Moisture assay of an antifungal by near-infrared diffuse reflectance spectroscopy.	2002 Apr 1	11861117
Breakthrough trichosporonosis in a bone marrow transplant recipient receiving caspofungin acetate.	2002 Aug 1	12115115
Invasive Aspergillus infections in hematologic malignancy patients.	2002 Jun	12070828
Safety and tolerability of caspofungin acetate in the treatment of fungal infections.	2002 Mar	12123423
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.	2004 Oct	15605126
Gateways to clinical trials.	2005 Jul-Aug	16179960
Caspofungin versus amphotericin B for candidemia: a pharmacoeconomic analysis.	2005 Jun	16117996
Gateways to clinical trials.	2005 Jun	16082422
Gateways to clinical trials.	2005 May	16082427
Fatal Blastoschizomyces capitatus sepsis in a neutropenic patient with acute myeloid leukemia: first documented case from Greece.	2005 May	15842341
Gateways to clinical trials.	2005 Nov	16357953
Candida glabrata prosthetic valve endocarditis treated successfully with fluconazole plus caspofungin without surgery: a case report and literature review.	2005 Nov	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 Nov	16275948
Gateways to clinical trials.	2005 Oct	16273137
Limitations of caspofungin in the treatment of obstructive pyonephrosis due to Candida glabrata infection.	2006 Aug 8	16895593
Gateways to clinical trials.	2006 Jul-Aug	16894408
Voriconazole in the management of nosocomial invasive fungal infections.	2006 Jun	18360588
Comparison of antifungal treatments for murine fusariosis.	2006 Nov	16973654
Gateways to clinical trials.	2006 Sep	17003851
Comedication of caspofungin acetate and cyclosporine A after allogeneic haematopoietic stem cell transplantation leads to negligible hepatotoxicity.	2008	18471157
Acute refractory hyperkalaemia and fatal cardiac arrest related to administration of liposomal amphotericin B.	2008 Nov	19011270
Gateways to clinical trials.	2008 Sep	18985183
Gateways to clinical trials.	2010 Jun	20664824
Recent advances in the treatment of mucormycosis.	2010 Nov	21308550
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.	2015 May 18	25811541

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 `Fri Dec 15 16:31:45 GMT 2023` Edited by `admin` on `Fri Dec 15 16:31:45 GMT 2023`
Record UNII	F0XDI6ZL63
Record Status	`Validated (UNII)`
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Name

Type

Language

CASPOFUNGIN

Official Name

English

caspofungin [INN]

Common Name

English

CASPOFUNGIN [HSDB]

Common Name

English

PNEUMOCANDIN B0, 1-((4R,5S)-5-((2-AMINOETHYL)AMINO)-N2-((10R,12S)-10,12-DIMETHYL-1-OXOTETRADECYL)-4-HYDROXY-L-ORNITHINE)-5-((3R)-3-HYDROXY-L-ORNITHINE)-

Systematic Name

English

L-743,872

Code

English

L-743872

Code

English

Caspofungin [WHO-DD]

Common Name

English

CASPOFUNGIN [EMA EPAR]

Common Name

English

CASPOFUNGIN [MI]

Common Name

English

CASPOFUNGIN [VANDF]

Common Name

English

(4R,5S)-5-((2-AMINOETHYL)AMINO)-N2-(10,12-DIMETHYLTETRADECANOYL)-4-HYDROXY-L-ORNITHYL-L-THREONYL-TRANS-4-HYDROXY-L-PROLYL-(S)-4-HYDROXY-4-(P-HYDROXYPHENYL)-L-THREONYL-THREO-3-HYDROXY-L-ORNITHYL-TRANS-3-HYDROXY-L-PROLINE CYCLIC (1->6) DISULFIDE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C514