Drug reference

Pertuzumab

Monoclonal Antibody · Antineoplastic

Monoclonal AntibodyAntineoplasticATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

1 major

incl. contraindicated

PREGNANCY

FDA category + note

Top interactionssee all 2 →

AnthracyclinesContraindicatedTextbookG&G 14e · p1419

Mechanism

Pertuzumab is a recombinant humanised monoclonal antibody that binds to the extracellular domain (subdomain II) of the human epidermal growth factor receptor 2 protein (HER2). This binding inhibits HER2 dimerisation and subsequently blocks HER2 intracellular signaling, thereby suppressing tumor cell growth.

Indications

HER2-positive early stage breast cancer (in combination with trastuzumab and chemotherapy)HER2-positive metastatic or locally recurrent unresectable breast cancer (in combination with trastuzumab and docetaxel)breast cancer (HER2 amplification; HER2 overexpression)gastric cancer (HER2 amplification; HER2 overexpression)HER2-positive metastatic breast cancer (in combination with trastuzumab and docetaxel)HER2-positive locally advanced, inflammatory, or early-stage breast cancer (in combination with trastuzumab and docetaxel)Approved for use in early-stage breast cancerFor HER2-positive tumors: neoadjuvant therapy (with or without trastuzumab for 4–5 months), followed by further pertuzumab to complete a year if pCR achievedFor smaller tumors (clinically node-negative, <3cm) with HER2-positive status, regimen of single-agent weekly paclitaxel for 12 weeks in conjunction with a year of trastuzumab (with or without pertuzumab)Adjuvant pertuzumab added to trastuzumab provides modest benefit

Dosing

Adult: Adult: (consult product literature or local protocols) BY INTRAVENOUS INFUSION

Pharmacokinetics

Half-life

18 days (median)

Contraindications

Conditions that could impair left ventricular function
History of congestive heart failure
Impaired left ventricular function
Prior anthracycline exposure
Radiotherapy to the chest area
Recent myocardial infarction
Serious cardiac arrhythmia
Uncontrolled hypertension

Side effects

Common

AlopeciaAnaemiaAppetite decreasedArthralgiaAstheniaChillsConstipationCoughCytokine release syndromeDiarrhoeaDizzinessDyspepsiaDyspnoeaExcessive tearingFeverHeadacheHypersensitivityIncreased risk of infectionInfusion related reactionInsomniaLeucopeniaMucositisMyalgiaNail disorderNauseaNeutropeniaOedemaPainPeripheral neuropathyRespiratory disordersSkin reactionsStomatitisTaste alteredVomitingFatigueLoose stools or diarrhea (manageable with loperamide)

Serious

Cardiotoxicity with reduced left ventricular function (leading to congestive heart failure)
Infusion related reaction
Hypersensitivity
Cytokine release syndrome
Myelosuppression (e.g., neutropenia, leucopenia, anaemia)
Increased risk of infection
cardiotoxicity (similar to trastuzumab)
embryofetal harm