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Drug reference

Letermovir

Cytomegalovirus terminase complex inhibitor (antiviral) · CMV prophylaxis

START
480 mg PO/IV once daily through day 100 post-HSCT
TYPICAL MAX
480 mg/day (240 mg/day if on cyclosporine)
STOP IF
Severe hypersensitivity
WATCH
Drug interactions (CYP3A4); LFTs if symptoms; CMV viral load
CDSCO approvedATC J05AX18
Dose laddermg/d
240w/ cyclosporine480standard
Renal dose adjustmenteGFR mL/min/1.73m²
FULLOral usual; avoid IV if CrCl <10 (vehicle)10CAUTIONUse oral; …90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1hONSET2.5hPEAK12h1dDURATION
ONSET
1h · absorption
PEAK
2.5h · Tmax
12h ·
DURATION
1d · once-daily
EXCRETION
Mainly faecal; <2% renal
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Use only if benefit outweighs risk; limited data.
FDA category + note
Top interactionssee all 12
  • PimozideContraindicatedDatabaseKimi deep-research + Cla
  • SimvastatinContraindicatedDatabaseKimi deep-research + Cla
  • AcalabrutinibSevereDatabaseDDInter
  • AlfentanilSevereDatabaseDDInter

Mechanism

Inhibits the CMV DNA terminase complex (pUL51/pUL56/pUL89), preventing viral DNA cleavage and packaging; selective for CMV (no activity against other herpesviruses, no nephro/marrow toxicity of older agents).

Indications

Prophylaxis of CMV infection/disease in adult CMV-seropositive recipients of allogeneic haematopoietic stem-cell transplantProphylaxis of CMV in selected solid-organ transplant recipients

Dosing

Adult
480 mg PO/IV once daily through day 100 post-transplant (with cyclosporine: reduce to 240 mg once daily).
Pediatric
Limited data; specialist.
Renal adjustment
No dose adjustment for any eGFR (oral). IV: avoid CrCl <10 due to vehicle accumulation.
Hepatic adjustment
Moderate impairment: no adjustment; severe: avoid (limited data).
Geriatric
No specific adjustment.
Max dose
480 mg once daily (240 mg with cyclosporine)

Pharmacokinetics

Onset
Antiviral effect within days
Peak effect
~1.5–3 h (Tmax)
Duration
~24 h (once-daily)
Half-life
~12 h
Bioavailability
~94% (with cyclosporine ~85%; tablet)
Protein binding
>99%
Metabolism
Mainly biliary excretion; minor UGT1A1/1A3 glucuronidation; CYP3A4 inhibitor/inducer
Excretion
Mainly faecal; <2% renal

Contraindications

  • Co-administration with pimozide / ergot alkaloids (CYP3A4 inhibition)
  • Co-administration with pitavastatin/simvastatin if also on cyclosporine
  • Hypersensitivity

Side effects

Common
Nausea/vomitingDiarrhoeaHeadacheCoughPeripheral oedemaFatigue
Serious
  • Hypersensitivity
  • Significant drug interactions (CYP3A4/UGT modulation)

Pregnancy & lactation

Pregnancy

Use only if benefit outweighs risk; limited data.

Lactation

Limited data; weigh benefit/risk.

Drug interactions

Pimozide
Contraindicated
Database

CYP3A4 inhibition

Contraindicated

Source: Kimi deep-research + Cla

Simvastatin
Contraindicated
Database

Marked OATP1B/CYP3A4 inhibition

Contraindicated in that combination

Source: Kimi deep-research + Cla

Acalabrutinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Alfentanil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Atorvastatin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Avanafil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Avapritinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Benzhydrocodone
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Berotralstat
Severe
Database

Drug interaction classified as: excretion

Source: DDInter

Bosutinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Brexpiprazole
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Brigatinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Ask House about Letermovir

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Sources: Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20