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Bortezomib

Proteasome inhibitor (boronic acid) · Antineoplastic

Also known as Velcade, PS-341

START
1.3 mg/m² SC days 1,4,8,11 q21d (per regimen); antiviral prophylaxis
TYPICAL MAX
1.3 mg/m²/dose
STOP IF
Grade ≥3 neuropathy/severe neuropathic pain, severe thrombocytopenia, cardiopulmonary deterioration
WATCH
Neuropathy grading each visit, platelets/CBC, zoster prophylaxis, hydration/TLS
CDSCO approvedSchedule HATC L01XG01
Dose laddermg/d
0.7start1titrate1.3standard per m²
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment at any eGFR incl. dialysis (give post-dialysis)90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
8minONSET30minPEAK4.2d3dDURATION
ONSET
8min · absorption onset
PEAK
30min · Cmax
4.2d · terminal t½ (multi-dose)
DURATION
3d · proteasome recovery
EXCRETION
Hepatic CYP3A4/2C19; metabolite excretion
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Avoid — embryo-fetal toxicity; effective contraception both sexes
FDA category + note
Top interactionssee all 12
  • Live VaccinesContraindicatedDatabaseKimi deep-research + Cla
  • AdalimumabSevereDatabaseDDInter
  • ApalutamideSevereDatabaseDDInter
  • BaricitinibSevereDatabaseDDInter
Available in India

47 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Reversible inhibition of the 26S proteasome chymotrypsin-like (β5) activity, causing accumulation of pro-apoptotic regulatory proteins (e.g. IκB → NF-κB suppression), ER stress and apoptosis, with particular sensitivity in plasma cells.

Indications

Multiple myelomaMantle cell lymphoma

Dosing

Adult
1.3 mg/m² SC (preferred) or IV on days 1,4,8,11 of 21-day cycles (schedule varies by regimen); weekly schedules used to reduce neuropathy.
Pediatric
Protocol-specific (specialist).
Renal adjustment
No adjustment for renal impairment/dialysis (give after dialysis).
Hepatic adjustment
Bilirubin >1.5×ULN: reduce starting dose to 0.7 mg/m², titrate by tolerance.
Geriatric
No specific adjustment; monitor neuropathy.
Max dose
1.3 mg/m²/dose (per schedule)

Pharmacokinetics

Onset
Proteasome inhibition within 1 h of dose
Peak effect
Cmax minutes (IV) ; SC similar exposure
Duration
Recovery of proteasome activity ~72 h
Half-life
~40–190 h (multi-compartment, after multiple dosing)
Bioavailability
SC bioavailability equivalent AUC to IV
Protein binding
~83%
Metabolism
Hepatic CYP3A4/2C19 (deboronation)
Excretion
Metabolite excretion; limited unchanged

Contraindications

  • Hypersensitivity to bortezomib, boron or mannitol
  • Intrathecal administration (fatal)
  • Severe hepatic impairment (dose-reduce, not absolute)

Side effects

Common
Peripheral sensory neuropathyThrombocytopenia (cyclical), anaemia, neutropeniaFatigue, nausea, diarrhoea/constipationPyrexia
Serious
  • Severe painful peripheral neuropathy
  • Severe thrombocytopenia → bleeding
  • Herpes zoster reactivation (give prophylaxis)
  • Cardiac failure / pulmonary toxicity (PRES, ILD rare)
  • Tumour lysis syndrome; hepatotoxicity

Pregnancy & lactation

Pregnancy

Avoid — embryo-fetal toxicity; effective contraception both sexes

Lactation

Do not breastfeed during and after therapy

Drug interactions

Live Vaccines
Contraindicated
Database

Immunosuppression

Avoid live vaccines

Source: Kimi deep-research + Cla

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Baricitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Carbamazepine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Certolizumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cladribine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clozapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Deferiprone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Drugs Causing Peripheral Neuropathy
Severe
Database

Additive neuropathy

Avoid combination; monitor neuro exam

Source: Kimi deep-research + Cla

Enzalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Etanercept
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Ask House about Bortezomib

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

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19