SYNONYM(S):

COMMON TRADE NAME(S):

ABRAXANE(r)

CLASSIFICATION: antimicrotubule agent,1 cytotoxic

Special pediatric considerations are noted when applicable, otherwise adult provisions apply.

MECHANISM OF ACTION:

This is a paclitaxel formulation that contains albumin (human) and is nanoparticle albumin-bound.1 See Paclitaxel Monograph for detailed mechanism of action.

PHARMACOKINETICS:

Distribution cross blood brain barrier? no information found
volume of distribution 632 L/m 2
plasma protein binding no information found
Metabolism hepatic via CYP2C8 and CYP3A4
active metabolite(s) 6a-hydroxypaclitaxel (major); 3 -p-hydroxypaclitaxel and 6a, 3 -p-dihydroxypaclitaxel (minor)
inactive metabolite(s) no information found
Excretion extensive non-renal clearance
urine unchanged drug (4%)
feces (20%)
terminal half life 27.4 h
clearance 15.2 L/h/m 2

Adapted from standard reference1 unless specified otherwise.

USES:

Primary uses: Other uses:

*Breast cancer, metastatic

*Health Canada approved indication

SPECIAL PRECAUTIONS1:

Do not administer if neutrophil counts are <1,500 cells/mm3 at baseline (equivalent to 1.5 x 109 cells/L). Do not substitute with or for other paclitaxel formulations. Theoretical risk of viral disease transmission, due to human albumin component, is extremely remote. Premedication to prevent hypersensitivity reactions is not required prior to administration. Contains no alcohol.

Carcinogenicity: 1

not studied

Mutagenicity: Paclitaxel nab is not mutagenic in Ames test and mammalian in vitro mutation test.1 It is clastogenic in mammalian in vitro and in vivo chromosome tests.

Fertility: 1

testicular atrophy/degeneration in male rats, and reduced fertility in untreated female mates

Pregnancy: FDA Pregnancy Category D.2 There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life- threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Breastfeeding 1

is not recommended due to the potential secretion into breast milk.

SIDE EFFECTS:

The table includes adverse events that presented during drug treatment but may not necessarily have a causal relationship with the drug. Because clinical trials are conducted under very specific conditions, the adverse event rates observed may not reflect the rates observed in clinical practice. Adverse events are generally included if they were reported in more than 1% of patients in the product monograph. When placebo-controlled trials are available, adverse events are included if the incidence is >5% higher in the treatment group.

ORGAN SITE SIDE EFFECT
allergy/immunology hypersensitivity reaction (1-4%)
blood/bone marrow/ febrile neutropenia anemia (20%)
febrile neutropenia (2%)
neutropenia (80%), may be severe
leucopenia (72%)
thrombocytopenia (2%)
cardiovascular (arrhythmia) abnormal ECG (all patients 60%, patients with abnormal baseline 35%)
cardiovascular (general) hypotension(5%); during infusion, often asymptomatic
severe cardiovascular events (3%), including chest pain, cardiac arrest, supraventricular tachycardia, edema, thrombosis, pulmonary thromboembolism, pulmonary emboli, and hypertension
constitutional symptoms asthenia (47%, severe 8%)
dermatology/skin extravasation hazard: irritant
alopecia (90%)
injection site reaction (1%)
nail changes (1%)
skin changes, transient including rash (9%), flushing 2%, pruritus 6%
gastrointestinal emetogenic potential: low 3
anorexia
constipation
dehydration
diarrhea (27%)
mucositis (7%)
nausea (30%)
vomiting (18%)
hemorrhage bleeding (2%)
infection fever (14%)
infections (24%); most frequently oral candidiasis, respiratory tract infection, pneumonia
ORGAN SITE SIDE EFFECT
metabolic/laboratory alkaline phosphatase elevations (36%)
ALT elevations (36%)
AST elevations (39%)
bilirubin elevations (7%)
GGT elevations (50%, severe 14%)
musculoskeletal arthralgia/myalgia (44%, severe 8%)
asthenia (47%)
neurology sensory neuropathy (71%, severe 10%)
ocular/visual ocular/visual disturbances (13%)
pulmonary see severe cardiovascular events in cardiovascular (general)
cough (7%)
dyspnea (12%)
fluid retention/edema (10%)
renal/genitourinary creatinine elevation (11%, severe <1%)

Adapted from standard reference1 unless specified otherwise.

INTERACTIONS:

Nab-paclitaxel 1

is metabolized by CYP2C8 and CYP3A4; caution should be exercised when administering with drugs which are CYP 2C8 or CYP3A4 inducers or inhibitors.

SUPPLY AND STORAGE:

Injection: Abraxis Oncology supplies the drug as a single use vial containing 100 mg of paclitaxel and approximately 900 mg of human albumin.1 Store vials in original containers at 20-25deg C. Protect from bright light.

For basic information on the current brand used at the BC Cancer Agency, see Chemotherapy Preparation and Stability Chart in Appendix.

SOLUTION PREPARATION AND COMPATIBILITY:

For basic information on the current brand used at the BC Cancer Agency, see Chemotherapy Preparation and Stability Chart in Appendix.

.

Additional information1: do NOT inject NS diluent directly onto powder or excessive foaming will occur allowing reconstituted solution to stand will enable wetting of powder if foaming or clumping occurs, stand solution for a minimum of 15 minutes until foam subsides reconstituted solution should be milky and homogenous without visible particles If visible particulates present, gently invert vial for complete resuspension prior to use latex-free stopper neither freezing nor refrigeration adversely affects the stability of the product

Compatibility: 1

Do not mix any other drugs.

PARENTERAL ADMINISTRATION:

BCCA administration guideline noted in bold , italics
Subcutaneous no information found
Intramuscular no information found
Direct intravenous no information found
Intermittent infusion over 30 min 1
Continuous infusion no information found
Intraperitoneal no information found
Intrapleural no information found
Intrathecal no information found
Intra-arterial no information found
Intravesical no information found

DOSAGE GUIDELINES:

Refer to protocol by which patient is being treated. Numerous dosing schedules exist and depend on disease, response and concomitant therapy. Guidelines for dosing also include consideration of absolute neutrophil count (ANC). Dosage may be reduced, delayed or discontinued in patients with bone marrow depression due to cytotoxic/radiation therapy or with other toxicities.

Adults: Cycle Length: BCCA usual dose noted in bold, italics Intravenous: 3 weeks1: 260 mg/m2 IV for one dose on day 1 Dose reductions:

0.5 x 109 cells/L) for a week or longer, or severe sensory neuropathy 180 mg/m2 for severe neutropenia or severe sensory neuropathy hold for grade 3 sensory neuropathy, until resolution to grade 1 or 2, followed by a dose reduction for all subsequent doses

Concurrent radiation:

no information found

Dosage in myelosuppression:

modify according to protocol by which patient is being treated; if no guidelines

available, refer to Appendix 6 "Dosage Modification for Myelosuppression" Dosage in renal failure: not studied1; in the randomized controlled trial, patients were excluded for baseline serum creatinine >2 mg/dL1 (equivalent to 177 mmol/L) Dosage in hepatic failure: not studied1; in the randomized controlled trial, patients were excluded for baseline serum bilirubin >1.5 mg/dL1

Dosage in dialysis:

no information found

REFERENCES:

  1. Abraxis Oncology. ABRAXANE(r) product monograph. Richmond Hill, Ontario; 26 June 2006.

Karen Law, B. Pharm. Personal communication. Product Director, Abraxis Oncology, A Division of Abraxis Bioscience, Inc; 6 September 2007.

BC Cancer Agency. (SCNAUSEA) Guidelines for Prevention and Treatment of Chemotherapy-induced Nausea and Vomiting in Adults. Vancouver, British Columbia: BC Cancer Agency; 1 November 2005.