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vismodegib

Hedgehog pathway inhibitor (SMO antagonist) · Antineoplastic agent

START
150 mg PO once daily (after pregnancy test in females of childbearing potential)
TYPICAL MAX
150 mg/day
STOP IF
Pregnancy, severe muscle / hepatic toxicity, or premature epiphyseal fusion (paediatric)
WATCH
Pregnancy testing prior + monthly; do not donate blood / semen during and 24 mo after
CDSCO approvedATC L01XJ01
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment at any eGFR90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1hONSET2.5hPEAK1.7w1dDURATION
ONSET
1h · absorption
PEAK
2.5h · Tmax
1.7w · t½ ~12 d (SS)
DURATION
1d · once-daily
EXCRETION
Mainly faecal (~82%); ~4% renal
route + CYP
INTERACTIONS
1 major
incl. contraindicated
PREGNANCY
Contraindicated — severe teratogen; pregnancy testing required; effective contraception during and 24 months after.
FDA category + note
Top interactionssee all 5
  • PregnancyContraindicatedDatabaseKimi deep-research + Cla · p1389

Mechanism

Selective small-molecule inhibitor of Smoothened (SMO), a transmembrane component of the Hedgehog signalling pathway — blocks aberrant pathway activation driving basal-cell carcinoma growth.

Indications

Metastatic basal-cell carcinomaLocally advanced basal-cell carcinoma not amenable to surgery / radiation

Dosing

Adult
150 mg PO once daily (with or without food).
Pediatric
Not approved (paediatric use restricted — premature epiphyseal fusion).
Renal adjustment
No specific adjustment.
Hepatic adjustment
Mild–moderate: no adjustment; severe: not studied.
Geriatric
No specific adjustment.
Max dose
150 mg/day

Pharmacokinetics

Onset
Tumour response over weeks–months
Peak effect
~2.4 h (Tmax)
Duration
~24 h (once-daily)
Half-life
~4 days (single dose); 12 days (steady state)
Bioavailability
~32%
Protein binding
>99%
Metabolism
Hepatic CYP2C9 / 3A4 minor (limited metabolism)
Excretion
Mainly faecal (~82%); ~4% renal

Contraindications

  • Pregnancy (severe teratogen — embryo-fetal death, malformations)
  • Hypersensitivity

Side effects

Common
Muscle spasmsAlopeciaDysgeusia (taste loss)Weight lossFatigueNausea/diarrhoea
Serious
  • Severe embryo-fetal toxicity (boxed)
  • Premature epiphyseal fusion (paediatric)
  • Severe rhabdomyolysis (rare)
  • Hepatotoxicity (rare)

Pregnancy & lactation

Pregnancy

Contraindicated — severe teratogen; pregnancy testing required; effective contraception during and 24 months after.

Lactation

Avoid breastfeeding during and 24 months after therapy; do NOT donate blood/semen during and 24 months after.

Drug interactions

Pregnancy
Contraindicated
Database

Severe teratogen (Hh pathway)

Contraindicated; strict contraception both sexes

Source: Kimi deep-research + Cla · p1389

Acid Suppressants
Moderate
Database

Reduced solubility

Avoid chronic acid suppression if possible

Source: Kimi deep-research + Cla

Drugs Causing Muscle Toxicity
Moderate
Database

Additive muscle effects

Monitor CK / muscle symptoms

Source: Kimi deep-research + Cla

Hepatotoxic Drugs
Moderate
Database

Additive hepatic injury

Monitor LFTs

Source: Kimi deep-research + Cla

P Gp Inhibitors
Moderate
Database

Possible increased vismodegib levels

Monitor for AEs

Source: Kimi deep-research + Cla

7 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

Ask House about vismodegib

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20