Fulvestrant

Registered South African indications: 

• Locally advanced or metastatic breast cancer
  - Disease relapse on or after adjuvant antioestrogen therapy
  - Disease progression on antioestrogen therapy

Contraindications 

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Breastfeeding
• Severe hepatic impairment

Cautions

• Severe renal impairment
• Mild to moderate hepatic impairment
• Bleeding disorders
• Thrombocytopaenia
• Patients at risk of thromboembolic events
• Dorsogluteal administration
• Osteoporosis
• Critical visceral disease
• Alcoholism
• Epilepsy
• May impair ability to drive and operate machinery

Forms available in SA and covered in this monograph: inj

Used for the treatment of 

• Oestrogen receptor positive, locally advanced or metastatic breast cancer in postmenopausal women
  - Not previously treated with endocrine therapy
  - Disease relapse on or after adjuvant antioestrogen therapy
  - Disease progression on antioestrogen therapy
• Adjuvant therapy in hormone receptor-positive, human epidermal growth factor receptor 2-negative locally advanced or metastatic breast cancer in women who have received prior endocrine therapy (additional agent/s required)
  - Combination treatment should be combined with a luteinising hormone releasing hormone agonist in pre-or perimenopausal women

Consult specialist for dosages and regimes

Not established for use in children below 18 years

Pregnancy

• Contraindicated
• Fulvestrant has been shown to cross the placenta after single intramuscular doses in rat and rabbit. Studies in animals have shown reproductive toxicity including an increased incidence of foetal abnormalities and deaths
• Patients of childbearing potential should use effective contraception during treatment with fulvestrant and for 2 years after the last dose
• If pregnancy occurs while taking fulvestrant, the patient must be informed of the potential hazard to the foetus and potential risk for loss of pregnancy

Breastfeeding

• Contraindicated
• Breastfeeding must be discontinued during treatment with fulvestrant
• Fulvestrant is excreted in milk in lactating rats. It is not known whether fulvestrant is excreted in human milk
• Considering the potential for serious adverse reactions due to fulvestrant in breastfed infants, use during breastfeeding is contraindicated

Fertility

• The effects of fulvestrant on fertility in humans has not been studied

Renal Impairment

• Mild to moderate (CrCl >30 ml/min): No dose adjustment recommended
• Severe (CrCl <30 ml/min): Caution; no information available
  Safety and efficacy have not been evaluated in severe renal impairment

Hepatic Impairment

• Mild to moderate (Child-Pugh Class A & B): Caution; no dose adjustment recommended 
• Severe (Child-Pugh Class C): Contraindicated

Elderly

• No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Prohibited - At all times

Central Nervous System Disorders

• Headache
• Asthenia
• Neuralgia
• Peripheral neuropathy
• Sciatica

Cardiovascular Disorders

• Venous thromboembolism
• Hot flushes

Gastrointestinal Disorders

• Nausea and vomiting
• Diarrhoea

Hepatobiliary Disorders

• Increased hepatic enzymes
• Increased bilirubin
• Hepatic failure
• Hepatitis
• Elevated gamma-glutamyltransferase

Genitourinary Disorders

• Urinary tract infections
• Vaginal moniliasis
• Leukorrhoea
• Vaginal haemorrhage

Endocrine and Metabolic Disorders

• Anorexia

Musculoskeletal Disorders

• Joint pain
• Musculoskeletal pain
• Arthralgia
• Myalgia
• Pain in extremity
• Back pain

Skin and Subcutaneous Tissue Disorders

• Rash
• Injection site reactions
• Injection site haemorrhage
• Injection site haematoma

Immune, Blood and Lymphatic System Disorders

• Reduced platelet count
• Hypersensitivity reactions
• Anaphylactic reactions

• Anticoagulants

• Hepatic function

None routine. Specific cases may require

• Pregnancy test

Fulvestrant is a competitive oestrogen receptor (ER) antagonist with an affinity comparable to oestradiol. Fulvestrant blocks the trophic actions of oestrogens without any partial agonist (oestrogen-like) activity. The mechanism of action is associated with downregulation of oestrogen receptor protein levels.

Injection (per 5ml) 250mg

• Eranfu 250 (Dr Reddy's Laboratories)
• Faslodex (AstraZeneca) originator
• Fastelev (Teva Pharmaceuticals)
• Fulvestrant Mylan (Mylan)