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

Stem definition	Drug id	CAS RN
antivirals	5262	917389-32-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: letermovir prevymis AIC246	Letermovir inhibits the CMV DNA terminase complex (pUL51, pUL56, and pUL89) which is required for viral DNA processing and packaging. Biochemical characterization and electron microscopy demonstrated that letermovir affects the production of proper unit length genomes and interferes with virion maturation. Genotypic characterization of virus resistant to letermovir confirmed that letermovir targets the terminase complex. Molecular weight: 572.56 Formula: C29H28F4N4O4 CLOGP: 6.92 LIPINSKI: 2 HAC: 8 HDO: 1 TPSA: 77.84 ALOGS: -4.76 ROTB: 7 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

letermovir
prevymis
AIC246

Letermovir inhibits the CMV DNA terminase complex (pUL51, pUL56, and pUL89) which is required for viral DNA processing and packaging. Biochemical characterization and electron microscopy demonstrated that letermovir affects the production of proper unit length genomes and interferes with virion maturation. Genotypic characterization of virus resistant to letermovir confirmed that letermovir targets the terminase complex.

Molecular weight: 572.56
Formula: C29H28F4N4O4
CLOGP: 6.92
LIPINSKI: 2
HAC: 8
HDO: 1
TPSA: 77.84
ALOGS: -4.76
ROTB: 7

Status: ONP

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

Drug dosage:

Dose	Unit	Route
0.48	g	O
0.48	g	P

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Bocci G, Oprea TI, Benet LZ
BA (Bioavailability)	0.94 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
S (Water solubility)	0.35 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company
Jan. 8, 2018	EMA	Merck Sharp & Dohme Limited
March 23, 2018	PMDA	MSD KK
Nov. 8, 2017	FDA	MERCK SHARP DOHME

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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
Cytomegalovirus infection reactivation	196.24	56.21	37	1068	3926	63483991
Off label use	91.44	56.21	82	1023	674380	62813537
Pathogen resistance	89.34	56.21	21	1084	6377	63481540
Cytomegalovirus viraemia	86.58	56.21	20	1085	5629	63482288
Post transplant lymphoproliferative disorder	57.22	56.21	14	1091	5017	63482900

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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
Cytomegalovirus infection reactivation	163.52	61.89	38	1279	5080	34950534
Off label use	108.86	61.89	103	1214	419421	34536193
Pathogen resistance	108.08	61.89	31	1286	9451	34946163
Oesophagitis	89.59	61.89	29	1288	13232	34942382
Encephalitis cytomegalovirus	63.02	61.89	12	1305	606	34955008

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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
Cytomegalovirus infection reactivation	333.65	50.82	72	2327	8644	79733345
Off label use	174.53	50.82	171	2228	907044	78834945
Pathogen resistance	174.35	50.82	47	2352	14295	79727694
Cytomegalovirus viraemia	132.52	50.82	37	2362	12784	79729205
Drug resistance	92.70	50.82	38	2361	42175	79699814
Oesophagitis	86.10	50.82	31	2368	24258	79717731
Cytomegalovirus infection	82.24	50.82	35	2364	42609	79699380
Thrombotic microangiopathy	68.69	50.82	25	2374	20144	79721845
Cystitis haemorrhagic	66.02	50.82	20	2379	9152	79732837
Encephalitis cytomegalovirus	64.15	50.82	13	2386	1137	79740852

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	J05AX18	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Other antivirals
FDA EPC	N0000193800	Cytomegalovirus DNA Terminase Complex Inhibitor
FDA MoA	N0000185507	Cytochrome P450 2C9 Inducers
FDA MoA	N0000185607	Cytochrome P450 2C19 Inducers
FDA MoA	N0000187062	Cytochrome P450 2C8 Inhibitors
FDA MoA	N0000190107	Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA	N0000190108	Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
FDA MoA	N0000193801	DNA Terminase Complex Inhibitors
MeSH PA	D000890	Anti-Infective Agents

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

Disease	Relation	SNOMED_ID	DOID
Cytomegalovirus infection	indication	28944009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	5.4	acidic
pKa2	6.77	Basic
pKa3	4.76	Basic

Orange Book patent data (new drug applications)

None

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
240MG	PREVYMIS	MERCK SHARP DOHME	N209939	Nov. 8, 2017	RX	TABLET	ORAL	Nov. 8, 2024	PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) INFECTION AND DISEASE IN ADULT CMV-SEROPOSITIVE RECIPIENTS [R+] OF AN ALLOGENEIC HEMATOPOIETIC STEM CELL TRANSPLANT (HSCT)
240MG	PREVYMIS	MERCK SHARP DOHME	N209939	Nov. 8, 2017	RX	TABLET	ORAL	June 5, 2026	PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) DISEASE IN ADULT KIDNEY TRANSPLANT RECIPIENTS AT HIGH RISK (DONOR CMV SEROPOSITIVE/RECIPIENT CMV SERONEGATIVE [D+/R-])
240MG	PREVYMIS	MERCK SHARP DOHME	N209939	Nov. 8, 2017	RX	TABLET	ORAL	June 5, 2030	FOR PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) DISEASE IN ADULT KIDNEY TRANSPLANT RECIPIENTS AT HIGH RISK (DONOR CMV SEROPOSITIVE/RECIPIENT CMV SERONEGATIVE [D+/R-])
240MG/12ML (20MG/ML)	PREVYMIS	MERCK SHARP DOHME	N209940	Nov. 8, 2017	RX	SOLUTION	INTRAVENOUS	Nov. 8, 2024	PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) INFECTION AND DISEASE IN ADULT CMV-SEROPOSITIVE RECIPIENTS [R+] OF AN ALLOGENEIC HEMATOPOIETIC STEM CELL TRANSPLANT (HSCT)
240MG/12ML (20MG/ML)	PREVYMIS	MERCK SHARP DOHME	N209940	Nov. 8, 2017	RX	SOLUTION	INTRAVENOUS	June 5, 2026	PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) DISEASE IN ADULT KIDNEY TRANSPLANT RECIPIENTS AT HIGH RISK (DONOR CMV SEROPOSITIVE/RECIPIENT CMV SERONEGATIVE [D+/R-])
240MG/12ML (20MG/ML)	PREVYMIS	MERCK SHARP DOHME	N209940	Nov. 8, 2017	RX	SOLUTION	INTRAVENOUS	June 5, 2030	FOR PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) DISEASE IN ADULT KIDNEY TRANSPLANT RECIPIENTS AT HIGH RISK (DONOR CMV SEROPOSITIVE/RECIPIENT CMV SERONEGATIVE [D+/R-])
480MG	PREVYMIS	MERCK SHARP DOHME	N209939	Nov. 8, 2017	RX	TABLET	ORAL	Nov. 8, 2024	PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) INFECTION AND DISEASE IN ADULT CMV-SEROPOSITIVE RECIPIENTS [R+] OF AN ALLOGENEIC HEMATOPOIETIC STEM CELL TRANSPLANT (HSCT)
480MG	PREVYMIS	MERCK SHARP DOHME	N209939	Nov. 8, 2017	RX	TABLET	ORAL	June 5, 2026	PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) DISEASE IN ADULT KIDNEY TRANSPLANT RECIPIENTS AT HIGH RISK (DONOR CMV SEROPOSITIVE/RECIPIENT CMV SERONEGATIVE [D+/R-])
480MG	PREVYMIS	MERCK SHARP DOHME	N209939	Nov. 8, 2017	RX	TABLET	ORAL	June 5, 2030	FOR PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) DISEASE IN ADULT KIDNEY TRANSPLANT RECIPIENTS AT HIGH RISK (DONOR CMV SEROPOSITIVE/RECIPIENT CMV SERONEGATIVE [D+/R-])
480MG/24ML (20MG/ML)	PREVYMIS	MERCK SHARP DOHME	N209940	Nov. 8, 2017	RX	SOLUTION	INTRAVENOUS	Nov. 8, 2024	PROPHYLAXIS OF CYTOMEGALOVIRUS (CMV) INFECTION AND DISEASE IN ADULT CMV-SEROPOSITIVE RECIPIENTS [R+] OF AN ALLOGENEIC HEMATOPOIETIC STEM CELL TRANSPLANT (HSCT)

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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
DNA terminase complex	Enzyme		TRM1_HCMVM TRM2_HCMVM TRM3_HCMVM	INHIBITOR	EC50	8.68		DRUG LABEL	DRUG LABEL

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External reference:

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ID	Source
017399	NDDF
1988648	RXNORM
1H09Y5WO1F	UNII
265515	MMSL
33254	MMSL
4037136	VANDF
45138674	PUBCHEM_CID
763033005	SNOMEDCT_US
763568003	SNOMEDCT_US
9384	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3075	TABLET, FILM COATED	240 mg	ORAL	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3075	TABLET, FILM COATED	240 mg	ORAL	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3075	TABLET, FILM COATED	240 mg	ORAL	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3076	TABLET, FILM COATED	480 mg	ORAL	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3076	TABLET, FILM COATED	480 mg	ORAL	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3076	TABLET, FILM COATED	480 mg	ORAL	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5003	INJECTION, SOLUTION	20 mg	INTRAVENOUS	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5003	INJECTION, SOLUTION	20 mg	INTRAVENOUS	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5003	INJECTION, SOLUTION	20 mg	INTRAVENOUS	NDA	31 sections
PREVYMIS	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5004	INJECTION, SOLUTION	20 mg	INTRAVENOUS	NDA	31 sections

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