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

Stem definition	Drug id	CAS RN
antibiotics, kanamycin and bekanamycin derivatives (obtained from Streptomyces kanamyceticus)	157	37517-28-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: amikacin amicacin amikacillin arikace lukadin amikacin sulfate amikacin hydrate	A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics. Molecular weight: 585.61 Formula: C22H43N5O13 CLOGP: -4.12 LIPINSKI: 3 HAC: 18 HDO: 13 TPSA: 331.94 ALOGS: -1.07 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

amikacin
amicacin
amikacillin
arikace
lukadin
amikacin sulfate
amikacin hydrate

A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.

Molecular weight: 585.61
Formula: C22H43N5O13
CLOGP: -4.12
LIPINSKI: 3
HAC: 18
HDO: 13
TPSA: 331.94
ALOGS: -1.07
ROTB: 10

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.59	g	Inhal.solution
1	g	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	98 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	25.61 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	2.40 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.88 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.16 L/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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Approvals:

Date	Agency	Company	Orphan
Jan. 22, 1981	FDA	APOTHECON
March 23, 2021	PMDA	Insmed GK

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
Drug resistance	357.50	18.62	152	15201	22781	63450888
Dysphonia	201.97	18.62	132	15221	47482	63426187
Pathogen resistance	190.94	18.62	68	15285	6330	63467339
Septic shock	153.80	18.62	128	15225	66501	63407168
Drug reaction with eosinophilia and systemic symptoms	151.30	18.62	97	15256	33739	63439930
Deafness	146.05	18.62	76	15277	17881	63455788
Multiple organ dysfunction syndrome	145.66	18.62	116	15237	56636	63417033
Therapy interrupted	127.94	18.62	86	15267	32369	63441300
Aphonia	115.90	18.62	54	15299	10009	63463660
Ototoxicity	114.81	18.62	32	15321	1330	63472339

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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
Drug resistance	313.15	16.61	180	16702	25747	34914302
Ototoxicity	251.29	16.61	74	16808	1843	34938206
Drug reaction with eosinophilia and systemic symptoms	171.91	16.61	136	16746	32876	34907173
Septic shock	160.03	16.61	185	16697	71649	34868400
Pathogen resistance	153.59	16.61	80	16802	9402	34930647
Rash maculo-papular	137.02	16.61	112	16770	28339	34911710
Deafness	132.64	16.61	77	16805	11188	34928861
Electrocardiogram QT prolonged	112.83	16.61	118	16764	40834	34899215
Drug ineffective	108.77	16.61	471	16411	456280	34483769
Product use in unapproved indication	101.79	16.61	194	16688	117305	34822744

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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
Drug resistance	570.04	16.65	284	27788	41929	79674387
Drug reaction with eosinophilia and systemic symptoms	340.90	16.65	236	27836	64008	79652308
Ototoxicity	338.74	16.65	98	27974	3176	79713140
Pathogen resistance	313.98	16.65	135	27937	14207	79702109
Septic shock	289.23	16.65	281	27791	122520	79593796
Rash maculo-papular	227.04	16.65	175	27897	55903	79660413
Deafness	216.30	16.65	118	27954	20919	79695397
Multiple organ dysfunction syndrome	210.81	16.65	235	27837	120011	79596305
Thrombocytopenia	186.09	16.65	334	27738	264925	79451391
Eosinophilia	169.44	16.65	135	27937	45210	79671106

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	D06AX12	DERMATOLOGICALS ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE ANTIBIOTICS FOR TOPICAL USE Other antibiotics for topical use
ATC	J01GB06	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE AMINOGLYCOSIDE ANTIBACTERIALS Other aminoglycosides
ATC	J01RA06	ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE COMBINATIONS OF ANTIBACTERIALS Combinations of antibacterials
ATC	S01AA21	SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFECTIVES Antibiotics
CHEBI has role	CHEBI:33281	antibiotics
CHEBI has role	CHEBI:36047	antibacterial drugs
CHEBI has role	CHEBI:61015	nephrotoxins
FDA CS	M0000946	Aminoglycosides
FDA EPC	N0000175477	Aminoglycoside Antibacterial
MeSH PA	D000900	Anti-Bacterial Agents

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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
Septicemia due to Escherichia coli	indication	9323009
Bacterial septicemia	indication	10001005	DOID:0040085
Infection due to Pseudomonas aeruginosa	indication	11218009
Staphylococcal meningitis	indication	12166008
Infection of skin AND/OR subcutaneous tissue	indication	19824006
Staphylococcal pneumonia	indication	22754005
Pneumonia due to Pseudomonas	indication	41381004
Pneumonia due to Escherichia coli	indication	51530003
Bacterial pneumonia	indication	53084003	DOID:874
Osteomyelitis	indication	60168000

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🐶 Veterinary Drug Use

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Species	Use	Relation
Dogs	Genitourinary tract infections caused by Escherichia coli	Indication
Dogs	Genitourinary tract infections caused by Proteus species	Indication
Dogs	Skin and soft tissue infections caused by Pseudomonas species	Indication
Dogs	Skin and soft tissue infections caused by Escherichia coli	Indication
Horses	Genital tract infections caused by Escherichia coli	Indication
Horses	Genital tract infections caused by Pseudomonas species	Indication
Horses	Genital tract infections caused by Klebsiella species	Indication

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🐶 Veterinary products

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Product	Applicant	Ingredients
Amiglyde-V	Zoetis Inc.	1
Amikacin Sulfate Injection	Cronus Pharma Specialities India Private Limited	1
AmiMax E Solution	Elanco US Inc.	1

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.04	acidic
pKa2	12.95	acidic
pKa3	13.39	acidic
pKa4	13.72	acidic
pKa5	9.4	Basic
pKa6	7.84	Basic
pKa7	7.41	Basic
pKa8	6.86	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	8802137	April 8, 2024	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS AS PART OF A COMBINATION DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	9827317	April 8, 2024	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS AS PART OF A COMBINATION ANTIBACTERIAL DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	7718189	June 6, 2025	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS AS PART OF A COMBINATION ANTIBACTERIAL DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	8632804	Dec. 5, 2026	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS WITH CYSTIC FIBROSIS AS PART OF A COMBINATION DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	8679532	Dec. 5, 2026	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS AS PART OF A COMBINATION ANTIBACTERIAL DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	9566234	Jan. 18, 2034	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS AS PART OF A COMBINATION ANTIBACTERIAL DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	10251900	May 15, 2035	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS AS PART OF A COMBINATION DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	10751355	May 15, 2035	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS AS PART OF A COMBINATION DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	11446318	May 15, 2035	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN ADULTS AS PART OF A COMBINATION DRUG REGIMEN
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	9895385	May 15, 2035	TREATING MYCOBACTERIUM AVIUM COMPLEX (MAC) LUNG DISEASE IN NON-CYSTIC FIBROSIS ADULTS AS PART OF A COMBINATION ANTIBACTERIAL DRUG REGIMEN

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	Sept. 28, 2025	TX OF MAC LUNG DISEASE IN ADULTS WITH LIMITED OR NO ALTERNATIVE TX OPTIONS AS PART OF A COMBO ANTIBACTERIAL DRUG REGIMEN WHO DO NOT ACHIEVE NEGATIVE SPUTUM CULTURES AFTER A MINIMUM OF 6 CONSECUTIVE MONTHS OF A MULTIDRUG BACKGROUND REGIMEN THERAPY
EQ 590MG BASE/8.4ML	ARIKAYCE KIT	INSMED INC	N207356	Sept. 28, 2018	RX	SUSPENSION, LIPOSOMAL	INHALATION	Sept. 28, 2030	GENERATING ANTIBIOTIC INCENTIVES NOW

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Macrolide 2'-phosphotransferase II; Macrolide 2'-phosphotransferase II protein MphB; Macrolide 2-phosphotransferase, mph(B)	Enzyme		O32553_ECOLX		Km	4.20		WOMBAT-PK

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External reference:

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ID	Source
AKN	PDB_CHEM_ID
002781	NDDF
004899	NDDF
10894	IUPHAR_LIGAND_ID
1269009	SNOMEDCT_US
2863	MMSL
3492	INN_ID
35287	MMSL
37768	PUBCHEM_CID
387266001	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6166	INJECTION	250 mg	INTRAMUSCULAR	ANDA	22 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6166	INJECTION	250 mg	INTRAMUSCULAR	ANDA	22 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6167	INJECTION	250 mg	INTRAMUSCULAR	ANDA	22 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	0641-6167	INJECTION	250 mg	INTRAMUSCULAR	ANDA	22 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	0703-9032	INJECTION, SOLUTION	500 mg	INTRAMUSCULAR	ANDA	20 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	0703-9040	INJECTION, SOLUTION	1 g	INTRAMUSCULAR	ANDA	20 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	23155-290	INJECTION, SOLUTION	250 mg	INTRAMUSCULAR	ANDA	20 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	23155-290	INJECTION, SOLUTION	250 mg	INTRAMUSCULAR	ANDA	20 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	23155-290	INJECTION, SOLUTION	250 mg	INTRAMUSCULAR	ANDA	20 sections
Amikacin Sulfate	HUMAN PRESCRIPTION DRUG LABEL	1	23155-785	INJECTION, SOLUTION	500 mg	INTRAMUSCULAR	ANDA	20 sections

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