Scroll

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

Stem definition	Drug id	CAS RN
systemic antifungal agents, miconazole derivatives	3483	171228-49-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: posaconazole noxafil posaconazol SCH 56592 SCH-56592	an antifungal medicine that belongs to the triazole group, it works by preventing the formation of ergosterol, which is an important part of fungal cell walls Molecular weight: 700.79 Formula: C37H42F2N8O4 CLOGP: 5.32 LIPINSKI: 2 HAC: 12 HDO: 1 TPSA: 111.79 ALOGS: -4.77 ROTB: 12 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

posaconazole
noxafil
posaconazol
SCH 56592
SCH-56592

an antifungal medicine that belongs to the triazole group, it works by preventing the formation of ergosterol, which is an important part of fungal cell walls

Molecular weight: 700.79
Formula: C37H42F2N8O4
CLOGP: 5.32
LIPINSKI: 2
HAC: 12
HDO: 1
TPSA: 111.79
ALOGS: -4.77
ROTB: 12

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.30	g	O
0.30	g	P

ADMET properties:

Show entries

Search:

Property	Value	Reference
BA (Bioavailability)	96 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	4.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	3.80 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	16.31 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	10.60 hours	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

Showing 1 to 9 of 9 entries

Previous1Next

Approvals:

Show entries

Search:

Date	Agency	Company
April 26, 2019	EMA	Accord Healthcare S.L.U.
Jan. 23, 2020	PMDA	MSD K.K.
Sept. 15, 2006	FDA	SCHERING

Showing 1 to 3 of 3 entries

Previous1Next

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
Febrile neutropenia	476.06	19.87	283	11019	118166	63359554
Pseudoaldosteronism	209.31	19.87	31	11271	44	63477676
Acute myeloid leukaemia	181.34	19.87	79	11223	17068	63460652
Septic shock	136.22	19.87	105	11197	66524	63411196
Neutropenia	133.69	19.87	160	11142	174845	63302875
Drug interaction	130.37	19.87	181	11121	228950	63248770
Graft versus host disease	122.87	19.87	46	11256	6717	63471003
Fusarium infection	115.09	19.87	26	11276	620	63477100
Hepatocellular injury	113.63	19.87	67	11235	27314	63450406
Cholestasis	111.72	19.87	68	11234	29366	63448354

Showing 1 to 10 of 137 entries

Previous1 2 3 4 5…14Next

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
Febrile neutropenia	315.91	17.02	349	15640	136500	34804442
Product use in unapproved indication	230.89	17.02	276	15713	117223	34823719
Aspergillus infection	176.90	17.02	94	15895	12160	34928782
Pseudoaldosteronism	159.05	17.02	28	15961	49	34940893
Bronchopulmonary aspergillosis	135.24	17.02	84	15905	14575	34926367
Septic shock	129.84	17.02	162	15827	71672	34869270
Acute myeloid leukaemia recurrent	127.69	17.02	45	15944	2125	34938817
Graft versus host disease	127.44	17.02	72	15917	10497	34930445
Mucormycosis	125.40	17.02	59	15930	5883	34935059
Fusarium infection	120.63	17.02	37	15952	1123	34939819

Showing 1 to 10 of 148 entries

Previous1 2 3 4 5…15Next

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
Febrile neutropenia	729.00	16.94	595	24741	230404	79488648
Pseudoaldosteronism	344.89	16.94	58	25278	118	79718934
Product use in unapproved indication	335.82	16.94	405	24931	249954	79469098
Neutropenia	253.06	16.94	379	24957	287331	79431721
Septic shock	252.41	16.94	249	25087	122552	79596500
Aspergillus infection	241.11	16.94	119	25217	19042	79700010
Mucormycosis	235.79	16.94	92	25244	8377	79710675
Acute myeloid leukaemia	221.19	16.94	132	25204	30753	79688299
Pneumonia fungal	207.61	16.94	91	25245	11119	79707933
Bronchopulmonary aspergillosis	204.51	16.94	112	25224	22182	79696870

Showing 1 to 10 of 252 entries

Previous1 2 3 4 5…26Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	J02AC04	ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE ANTIMYCOTICS FOR SYSTEMIC USE Triazole and tetrazole derivatives
CHEBI has role	CHEBI:36335	trypanocidal drugs
FDA CS	M0002083	Azoles
FDA EPC	N0000175487	Azole Antifungal
MeSH PA	D058888	14-alpha Demethylase Inhibitors
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000935	Antifungal Agents
MeSH PA	D000977	Antiparasitic Agents
MeSH PA	D000981	Antiprotozoal Agents
MeSH PA	D065607	Cytochrome P-450 Enzyme Inhibitors

Showing 1 to 10 of 15 entries

Previous1 2Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Mycosis	indication	3218000	DOID:1564
Coccidioidomycosis	indication	60826002	DOID:13450
Fusarium infection	indication	64250002
Aspergillosis	indication	65553006	DOID:13564
Mucormycosis	indication	76627001
Candidiasis	indication	78048006	DOID:1508
Candidiasis of mouth	indication	79740000	DOID:14262
Chromoblastomycosis	indication	187079000
Pharyngeal candidiasis	indication	240704003
Mycetoma	indication	410039003	DOID:13078

Showing 1 to 10 of 10 entries

Previous1Next

🐶 Veterinary Drug Use

Show entries

Search:

Species	Use	Relation
Dogs	Otitis externa caused by yeast, Malassezia pachydermatis	Indication
Dogs	Otitis externa associated with bacteria coagulase positive staphylococci	Indication
Dogs	Otitis externa associated with Pseudomonas aeruginosa	Indication
Dogs	Otitis externa associated with Enterococcus faecalis	Indication

Showing 1 to 4 of 4 entries

Previous1Next

🐶 Veterinary products

Product	Applicant	Ingredients
Posatex Otic Suspension	Intervet Inc.	3

Acid dissociation constants calculated using MoKa v3.0.0

Show entries

Search:

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.68	acidic
pKa2	5.12	Basic
pKa3	5.0	Basic
pKa4	2.66	Basic
pKa5	0.3	Basic

Showing 1 to 5 of 5 entries

Previous1Next

Orange Book patent data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
300MG/16.7ML (18MG/ML)	NOXAFIL	MERCK SHARP DOHME	N205596	March 13, 2014	RX	SOLUTION	INTRAVENOUS	9358297	June 24, 2031	PROPHYLAXIS OF INVASIVE ASPERGILLUS AND CANDIDA INFECTIONS IN ADULTS AND PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WHO ARE SEVERELY IMMUNOCOMPROMISED
300MG/16.7ML (18MG/ML)	NOXAFIL	MERCK SHARP DOHME	N205596	March 13, 2014	RX	SOLUTION	INTRAVENOUS	9358297	June 24, 2031	TREATMENT OF INVASIVE ASPERGILLOSIS IN ADULTS AND PEDIATRIC PATIENTS 13 YEARS OF AGE AND OLDER
300MG/16.7ML (18MG/ML)	NOXAFIL	MERCK SHARP DOHME	N205596	March 13, 2014	RX	SOLUTION	INTRAVENOUS	9023790	July 4, 2031	PROPHYLAXIS OF INVASIVE ASPERGILLUS AND CANDIDA INFECTIONS
300MG/16.7ML (18MG/ML)	NOXAFIL	MERCK SHARP DOHME	N205596	March 13, 2014	RX	SOLUTION	INTRAVENOUS	9023790	July 4, 2031	PROPHYLAXIS OF INVASIVE ASPERGILLUS AND CANDIDA INFECTIONS IN ADULTS AND PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WHO ARE SEVERELY IMMUNOCOMPROMISED
300MG/16.7ML (18MG/ML)	NOXAFIL	MERCK SHARP DOHME	N205596	March 13, 2014	RX	SOLUTION	INTRAVENOUS	9023790	July 4, 2031	TREATMENT OF INVASIVE ASPERGILLOSIS IN ADULTS AND PEDIATRIC PATIENTS 13 YEARS OF AGE AND OLDER

Showing 1 to 5 of 5 entries

Previous1Next

Orange Book exclusivity data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	NOXAFIL	MERCK SHARP DOHME	N205053	Nov. 25, 2013	RX	TABLET, DELAYED RELEASE	ORAL	May 31, 2024	NEW PATIENT POPULATION
100MG	NOXAFIL	MERCK SHARP DOHME	N205053	Nov. 25, 2013	RX	TABLET, DELAYED RELEASE	ORAL	June 17, 2024	FOR THE TREATMENT OF INVASIVE ASPERGILLOSIS IN PATIENTS 13 YEARS OF AGE AND OLDER
100MG	NOXAFIL	MERCK SHARP DOHME	N205053	Nov. 25, 2013	RX	TABLET, DELAYED RELEASE	ORAL	June 17, 2028	FOR THE TREATMENT OF INVASIVE ASPERGILLOSIS IN ADULTS AND PEDIATRIC PATIENTS 13 YEARS OF AGE AND OLDER
300MG	NOXAFIL POWDERMIX KIT	MSD MERCK CO	N214770	May 31, 2021	RX	FOR SUSPENSION, DELAYED RELEASE	ORAL	May 31, 2024	NEW PRODUCT
300MG/16.7ML (18MG/ML)	POSACONAZOLE	PAR STERILE PRODUCTS	A208768	May 25, 2022	RX	SOLUTION	INTRAVENOUS	Dec. 26, 2023	PATENT CHALLENGE
300MG/16.7ML (18MG/ML)	NOXAFIL	MERCK SHARP DOHME	N205596	March 13, 2014	RX	SOLUTION	INTRAVENOUS	May 31, 2024	NEW PATIENT POPULATION
300MG/16.7ML (18MG/ML)	NOXAFIL	MERCK SHARP DOHME	N205596	March 13, 2014	RX	SOLUTION	INTRAVENOUS	June 17, 2024	FOR THE TREATMENT OF INVASIVE ASPERGILLOSIS IN PATIENTS 13 YEARS OF AGE AND OLDER
300MG/16.7ML (18MG/ML)	NOXAFIL	MERCK SHARP DOHME	N205596	March 13, 2014	RX	SOLUTION	INTRAVENOUS	June 17, 2028	FOR THE TREATMENT OF INVASIVE ASPERGILLOSIS IN ADULTS AND PEDIATRIC PATIENTS 13 YEARS OF AGE AND OLDER

Showing 1 to 8 of 8 entries

Previous1Next

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
7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase	Enzyme	Q9UNU6	CP8B1_HUMAN		IC50	5.42	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN				WOMBAT-PK
Lanosterol 14-alpha demethylase	Enzyme		CP51_CANAL	INHIBITOR	MIC	9.40	WOMBAT-PK	CHEMBL
14-alpha sterol demethylase Cyp51A	Enzyme		Q4WNT5_ASPFU		Kd	5.57	CHEMBL
14-alpha sterol demethylase	Enzyme		Q96W81_ASPFM		Kd	7.14	CHEMBL
Sterol 14-alpha demethylase	Enzyme		CP51_TRYCC		IC50	7.32	CHEMBL
Sterol 14-alpha-demethylase	Enzyme		A0A2P2HJL8_ASPFA		Kd	6.88	CHEMBL
14-alpha sterol demethylase	Enzyme		G4WW85_ASPNG		Kd	6.88	CHEMBL
14-alpha sterol demethylase	Enzyme		Q9P8R0_ASPFM		Kd	6.88	CHEMBL

Showing 1 to 10 of 10 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
X2N	PDB_CHEM_ID
011210	NDDF
11428	IUPHAR_LIGAND_ID
21768	MMSL
282446	RXNORM
320488	MMSL
4025699	VUID
4025699	VANDF
420282006	SNOMEDCT_US
421747003	SNOMEDCT_US

Showing 1 to 10 of 22 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-1328	SUSPENSION	40 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-1328	SUSPENSION	40 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-1328	SUSPENSION	40 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-1328	SUSPENSION	40 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-2224	POWDER, FOR SUSPENSION	300 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-2224	POWDER, FOR SUSPENSION	300 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-2224	POWDER, FOR SUSPENSION	300 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-2224	POWDER, FOR SUSPENSION	300 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-4324	TABLET, COATED	100 mg	ORAL	NDA	31 sections
NOXAFIL	HUMAN PRESCRIPTION DRUG LABEL	1	0085-4324	TABLET, COATED	100 mg	ORAL	NDA	31 sections

Showing 1 to 10 of 30 entries

Previous1 2 3Next