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Abatacept

Class: Disease-modifying Antirheumatic Drugs
- Disease-modifying Antirheumatic Drugs
- DMARDs
Chemical Name: Fusion protein with an extracellular domain of human cytotoxic T-lymphocyte-associated antigen (CTLA-4) and modified Fc domain of human immunoglobulin G1
Molecular Formula: C1965H3080N479O695S16
CAS Number: 332348-12-6
Brands: Orencia

Medically reviewed by Drugs.com on Feb 1, 2021. Written by ASHP.

Introduction

Biologic response modifier and disease-modifying antirheumatic drug (DMARD); a recombinant fusion protein.

Uses for Abatacept

Rheumatoid Arthritis

Management of moderately to severely active rheumatoid arthritis in adults. Can be used alone or with conventional (nonbiologic) DMARDs.

Concomitant use with potent immunosuppressive agents such as biologic DMARDs (e.g., tumor necrosis factor [TNF; TNF-α] blocking agents) and Janus kinase (JAK) inhibitors is not recommended. (See Infectious Complications under Cautions and see Specific Drugs and Laboratory Tests under Interactions.)

Juvenile Arthritis

Management of moderately to severely active polyarticular course juvenile idiopathic arthritis in pediatric patients ≥2 years of age. Can be used alone or with methotrexate.

Concomitant use with potent immunosuppressive agents such as biologic DMARDs (e.g., TNF blocking agents) and JAK inhibitors is not recommended. (See Infectious Complications under Cautions and see Specific Drugs and Laboratory Tests under Interactions.)

Psoriatic Arthritis

Management of active psoriatic arthritis in adults. Can be used alone or with conventional (nonbiologic) DMARDs.

Concomitant use with potent immunosuppressive agents such as biologic DMARDs (e.g., TNF blocking agents) and JAK inhibitors is not recommended. (See Infectious Complications under Cautions and see Specific Drugs and Laboratory Tests under Interactions.)

Abatacept Dosage and Administration

Administration

Administer by IV infusion or sub-Q injection. In children 2 to <6 years of age with polyarticular course juvenile idiopathic arthritis, administer by sub-Q injection only.

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Commercially available for IV use as a lyophilized powder that must be reconstituted and diluted prior to administration.

Administer by IV infusion. Complete infusion within 24 hours of reconstitution.

Administer with an in-line, sterile, nonpyrogenic, low-protein-binding filter with a pore diameter ≤1.2 µm.

Consult manufacturer’s labeling for additional information on reconstitution, dilution, and administration.

Reconstitution

Reconstitute the appropriate number of vials containing 250 mg of abatacept lyophilized powder with 10 mL of sterile water for injection to provide a solution containing 25 mg/mL.

Use only the silicone-free disposable syringe provided by the manufacturer and an 18- to 21-gauge needle. If a siliconized syringe is inadvertently used, discard the solution since translucent particles may develop. If silicone-free disposable syringe is dropped or becomes contaminated, use a new silicone-free disposable syringe; may obtain additional syringes from manufacturer (800-673-6242 [800-ORENCIA]).

Direct sterile water for injection toward the side of the vial during reconstitution; swirl gently to minimize foaming. Do not shake; avoid prolonged or vigorous agitation. Upon dissolution, insert a vented needle into the vial to dissipate foam. Must be diluted further before IV administration.

Dilution

Remove the volume of diluent equal to the total required volume of reconstituted abatacept solution from a 100 mL bag of 0.9% sodium chloride injection.

Using same silicone-free disposable syringe used for reconstitution, slowly add reconstituted abatacept to the bag to a total volume of 100 mL. Mix gently; do not shake. Final concentration depends on amount of abatacept added but will be not exceed 10 mg/mL.

Discard any unused portion of reconstituted solution.

Rate of Administration

Infuse over 30 minutes.

Subcutaneous Administration

Commercially available for sub-Q use in single-use prefilled syringes and auto-injectors. Prefilled syringes and auto-injectors are not intended for IV administration.

Intended for sub-Q use under the guidance and supervision of a clinician, but may be self-administered if the clinician determines that the patient and/or their caregiver is competent to safely administer the drug by sub-Q injection after appropriate training and with medical follow-up as necessary. Pediatric patients may self-administer the sub-Q formulation if both the clinician and caregiver determine that self-administration is appropriate. Manufacturer states that the ability of pediatric patients to use the auto-injector has not been tested.

Allow the refrigerated prefilled syringe or auto-injector to sit at room temperature for 30 minutes prior to administration; do not warm the solution in any other way (e.g., microwave, immersion in warm water). Do not remove needle cover while drug is warming to room temperature.

Administer sub-Q injections into anterior thigh or abdomen; do not make abdominal injections within 5.08 cm (2 inches) of the umbilicus. May be administered into the upper outer arm by a caregiver. Inject the full amount of solution in the prefilled syringe or auto-injector. Rotate injection sites. Do not make injections into areas where the skin is tender, bruised, red, scaly, or hard, or into scars or stretch marks.

Dosage

Pediatric Patients

Juvenile Arthritis
IV

Pediatric patients ≥6 years of age weighing <75 kg: 10 mg/kg at 0, 2, and 4 weeks, then every 4 weeks.

Pediatric patients ≥6 years of age weighing ≥75 kg: Use adult dosage.

Sub-Q

Initiate sub-Q regimen without an IV loading dose.

Pediatric patients ≥2 years of age weighing 10 to <25 kg: 50 mg once weekly.

Pediatric patients ≥2 years of age weighing 25 to <50 kg: 87.5 mg once weekly.

Pediatric patients ≥2 years of age weighing ≥50 kg: 125 mg once weekly.

Adults

Rheumatoid Arthritis
IV

Adults weighing <60 kg: 500 mg at 0, 2, and 4 weeks, then every 4 weeks.

Adults weighing 60–100 kg: 750 mg at 0, 2, and 4 weeks, then every 4 weeks.

Adults weighing >100 kg: 1 g at 0, 2, and 4 weeks, then every 4 weeks.

Sub-Q

125 mg once weekly.

May administer a single optional loading dose by IV infusion within one day prior to the initial sub-Q dose; if IV loading dose is used, recommended dose is 500 mg in those weighing <60 kg, 750 mg in those weighing 60–100 kg, and 1 g in those weighing >100 kg.

To switch from IV to sub-Q therapy, administer initial sub-Q dose in place of next scheduled IV dose.

Psoriatic Arthritis
IV

Adults weighing <60 kg: 500 mg at 0, 2, and 4 weeks, then every 4 weeks.

Adults weighing 60–100 kg: 750 mg at 0, 2, and 4 weeks, then every 4 weeks.

Adults weighing >100 kg: 1 g at 0, 2, and 4 weeks, then every 4 weeks.

Sub-Q

125 mg once weekly.

IV loading dose is not required.

To switch from IV to sub-Q therapy, administer initial sub-Q dose in place of next scheduled IV dose.

Prescribing Limits

Pediatric Patients

Juvenile Arthritis
IV

Children ≥6 years of age weighing ≥75 kg: Maximum dose is 1 g.

Special Populations

No special population dosage recommendations at this time.

Cautions for Abatacept

Contraindications

None known.

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity reactions (e.g., anaphylaxis, angioedema), including life-threatening or fatal events, reported. Fatal anaphylaxis has occurred after the initial IV infusion and angioedema has occurred after the initial dose or with subsequent doses; onset of angioedema has occurred within hours of administration but sometimes has been delayed (i.e., by days).

Other allergic reactions (e.g., hypotension, urticaria, dyspnea) also reported.

Ensure appropriate measures for treatment of hypersensitivity reactions are readily available for use. If anaphylactic or other serious hypersensitivity reaction occurs, immediately stop administration and permanently discontinue use.

Infectious Complications

Possibility exists for agents that inhibit T-cell activation, including abatacept, to affect host defenses against infection.

Serious and sometimes fatal infections (including sepsis, pneumonia, cellulitis, urinary tract infections, bronchitis, diverticulitis, and acute pyelonephritis) reported, particularly in patients receiving concomitant immunosuppressive agents.

Concomitant use of abatacept and TNF blocking agents, other biologic antirheumatic therapies, or JAK inhibitors is not recommended. Monitor patients being switched from TNF blocking agents to abatacept for infection. (See Specific Drugs and Laboratory Tests under Interactions.)

Discontinue abatacept if serious infection develops. Closely monitor patients who develop new infections.

Use caution in patients with a history of recurring infections, underlying conditions that may predispose them to infections, or chronic, latent, or localized infections.

Evaluate all patients for active or latent tuberculosis prior to initiation of abatacept therapy. When indicated, initiate appropriate antimycobacterial regimen for the treatment of latent tuberculosis infection prior to abatacept.

HBV Reactivation

Use of antirheumatic drugs associated with reactivation of HBV infection in patients who are chronic carriers of the virus (i.e., hepatitis B surface antigen-positive [HBsAg-positive]). Screen patients at risk prior to initiation of therapy.

Immunization

Vaccine efficacy may be reduced. Patients may receive inactivated vaccines, but avoid live virus vaccines during abatacept therapy or within 3 months after discontinuance of the drug. (See Vaccines under Interactions and see Pediatric Use under Cautions.)

Update immunizations according to current administration guidelines prior to initiating abatacept therapy.

COPD

Possible exacerbations of COPD, cough, rhonchi, and dyspnea.

Use with caution; careful monitoring recommended for worsening of respiratory function.

Malignancies and Lymphoproliferative Disorders

Possibility exists for agents that inhibit T-cell activation, including abatacept, to affect host defenses against malignancies.

Lymphoma and lung cancer reported more frequently in patients with rheumatoid arthritis receiving IV abatacept versus control. Rheumatoid arthritis patients, especially those with highly active disease, may be at increased risk of lymphoma.

Other malignancies (e.g., myelodysplastic syndrome, melanoma, breast, bile duct, bladder, cervical, endometrial, ovarian, prostate, renal, thyroid, uterine, and nonmelanoma skin cancer) also reported.

Role of abatacept in the development and course of malignancies not fully determined.

Periodic dermatologic evaluations recommended for all patients receiving abatacept, particularly those at increased risk for skin cancer.

Blood Glucose Testing

Parenteral preparations containing maltose, including abatacept lyophilized powder for IV infusion, may cause falsely elevated results in blood glucose determinations that use glucose dehydrogenase pyrroloquinolinequinone (GDH-PQQ). (See Specific Drugs and Laboratory Tests under Interactions.)

Abatacept injection for sub-Q use does not contain maltose; therefore, no special glucose monitoring precautions required in patients receiving this formulation.

Immunogenicity

Development of antibodies to abatacept, including neutralizing antibodies, reported; no apparent effect on safety, efficacy, or pharmacokinetics of the drug. No serious acute infusion-related reactions observed in pediatric patients who resumed abatacept therapy following treatment interruption for up to 6 months.

Specific Populations

Pregnancy

No adequate and well-controlled studies of abatacept in pregnant women. Available data are insufficient to inform a drug-associated risk.

Not known whether abatacept crosses the placenta in humans.

Pregnancy registry at 877-311-8972.

No embryotoxicity or fetal malformations observed in animal studies; however, effects on immune function (i.e., increase in T-cell-dependent antibody response, thyroiditis) observed in female offspring in a prenatal and postnatal development study in rats. Unknown whether immunologic effects in rats are indicative of risk for autoimmune disease development in humans exposed to abatacept in utero. Exposure to abatacept in juvenile rats (may be more representative of the fetal human immune system) resulted in immune system abnormalities including inflammation of the thyroid and pancreas. (See Pediatric Use under Cautions.)

Safety of administering live vaccines to infants exposed to abatacept in utero is unknown; consider risks and benefits.

Lactation

Distributed into milk in rats; not known whether abatacept distributes into human milk, affects nursing infants, or affects milk production.

Pediatric Use

Safety and efficacy for the management of polyarticular course juvenile idiopathic arthritis established in pediatric patients ≥2 years of age; may be used as monotherapy or in combination with methotrexate.

Use of IV abatacept for management of polyarticular course juvenile idiopathic arthritis is supported by a randomized-withdrawal study evaluating efficacy, safety, and pharmacokinetics of IV abatacept in 190 pediatric patients 6–17 years of age; IV administration not evaluated in children <6 years of age.

Use of sub-Q abatacept for management of polyarticular course juvenile idiopathic arthritis is supported by an open-label pharmacokinetic and safety study of sub-Q abatacept in 205 pediatric patients 2–17 years of age and evidence of efficacy for IV abatacept in pediatric patients with juvenile idiopathic arthritis and for sub-Q abatacept in adults with rheumatoid arthritis.

Adverse effects reported in children similar to those reported in adults.

Safety and efficacy of abatacept not established in pediatric patients <2 years of age or for pediatric uses other than polyarticular course juvenile idiopathic arthritis.

In juvenile rats, administration of abatacept prior to immune system maturity was associated with increased incidence of fatal infections, changes in T-cell subsets (e.g., increased T-helper cells, decreased T-regulatory cells), and inhibition of T-cell-dependent antibody responses; lymphocytic inflammation of the thyroid and pancreatic islets also observed once these animals reached adulthood. Relevance of these findings to humans is unknown since rat immune system is undeveloped in the first few weeks after birth. In studies in adult mice and monkeys, inhibition of T-cell-dependent antibody responses was observed, but increased infection and mortality rates, altered T-helper cells, and inflammation of the thyroid and pancreas were not observed.

Review vaccination status of the child and administer all age-appropriate vaccines prior to initiation of abatacept.

Safety of administering live vaccines to infants exposed to abatacept in utero is unknown; consider risks and benefits.

Geriatric Use

No overall differences in efficacy or safety observed between geriatric patients ≥65 years of age and younger adults, but increased sensitivity of some older patients cannot be ruled out.

Possible increased incidence of infections and malignancies in geriatric patients; use with caution. (See Infectious Complications and also Malignancies and Lymphoproliferative Disorders under Cautions.)

Common Adverse Effects

Upper respiratory infection, nasopharyngitis, headache, nausea. Adverse effects generally similar following IV infusion or sub-Q injection.

Interactions for Abatacept

Vaccines

Avoid live virus vaccines. No data available on secondary transmission of infection by live virus vaccines in abatacept-treated patients.

Since abatacept may interfere with the immune response to antigens, vaccine efficacy may be reduced in patients receiving the drug. (See Immunization under Cautions and see Pediatric Use under Cautions.)

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

Biologic antirheumatic drugs (e.g., TNF blocking agents)

Insufficient experience to assess safety and efficacy of concomitant use

TNF blocking agents: Increased incidence of infection and serious infection, with no substantial increase in efficacy, observed with concomitant use compared with use of TNF blocking agent alone

Concomitant use not recommended (see Infectious Complications under Cautions)

Corticosteroids

No effect on clearance of abatacept

JAK inhibitors

Insufficient experience to establish safety and efficacy of concomitant use

Concomitant use not recommended

Methotrexate

No effect on clearance of abatacept

NSAIAs

No effect on clearance of abatacept

Tests for glucose

Maltose contained in abatacept lyophilized powder for IV infusion may interfere with blood glucose monitoring systems based on glucose dehydrogenase pyrroloquinolinequinone (GDH-PQQ) and cause falsely elevated blood glucose results

Abatacept for IV infusion: Use only glucose-specific test methods not affected by maltose (e.g., glucose dehydrogenase nicotine adenine dinucleotide [GDH-NAD], glucose oxidase, glucose hexokinase)

Abatacept injection for sub-Q use: Does not contain maltose; no special glucose monitoring precautions required

Abatacept Pharmacokinetics

Absorption

Bioavailability

Following multiple IV infusions in adults with rheumatoid arthritis, steady-state serum concentrations reached by day 60. No apparent systemic accumulation. AUC and peak serum concentrations are dose proportional over dose range of 2–10 mg/kg.

Steady-state concentrations reached by day 57 in adults with psoriatic arthritis receiving recommended IV weight-based dosages or weekly 125-mg sub-Q doses.

Following sub-Q administration, pharmacokinetics are linear and absolute bioavailability is approximately 79%.

Elimination

Half-life

Terminal half-life following IV or sub-Q administration is approximately 13–14 days in adults with rheumatoid arthritis.

Special Populations

Age and gender (adjusted for body weight) do not affect clearance.

Clearance increases with increasing body weight.

Pharmacokinetics not evaluated in patients with hepatic or renal impairment.

Stability

Storage

Parenteral

Powder for Injection, for IV Infusion

2–8°C in the original container; protect from light.

Store fully diluted solution at either room temperature or between 2–8°C. Discard if not used within 24 hours of reconstitution.

Injection, for Sub-Q Use

2–8°C in the original carton; protect from light. Do not freeze. During travel, store in cool carrier at 2–8°C.

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility

Compatible

Sodium chloride 0.9%.

Drug Compatibility

Information on the physical and/or chemical compatibility with other drugs is not available.

Actions

  • Inhibits T-cell activation by binding to CD80 and CD86, further blocking interaction with CD28.

  • Decreases T-cell proliferation and inhibits production of TNFα, interferon-γ and IL–2.

  • Suppresses inflammation, decreases anti-collagen antibody production, and reduces antigen specific production of interferon-γ.

Advice to Patients

  • Importance of providing patient a copy of the manufacturer’s patient information.

  • Importance of advising patients that concomitant use of abatacept and other potent immunosuppressive agents (e.g., biologic DMARDs, JAK inhibitors) is not recommended.

  • Importance of immediately informing a clinician if signs or symptoms of an allergic reaction (e.g., urticaria, difficulty breathing, swelling of the face, eyelids, or lips) occur on the day of or the day after abatacept administration.

  • Risk of serious infectious complications. Importance of patients informing clinicians promptly if any signs or symptoms of infection occur.

  • Importance of avoiding live vaccines during abatacept therapy and for 3 months following discontinuance of the drug.

  • Advise patients that the IV formulation of abatacept contains maltose and may cause falsely elevated glucose readings when blood glucose monitoring systems based on glucose dehydrogenase pyrroloquinolinequinone (GDH-PQQ) are used; importance of using glucose-specific test methods not affected by maltose.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Importance of encouraging pregnant women who have been exposed to abatacept to enroll in the manufacturer's pregnancy registry.

  • Importance of instructing the patient and/or caregiver regarding proper dosage and administration of abatacept, including the use of aseptic technique, and proper disposal of prefilled syringes and auto-injectors if it is determined that the patient and/or caregiver is competent to safely administer sub-Q injections of the drug.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any other illnesses (e.g., COPD; concomitant or recurrent infections; history of cancer, tuberculosis, or HBV infection).

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Abatacept

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

For injection, for IV infusion

250 mg

Orencia (with a silicone-free disposable syringe)

Bristol-Myers Squibb

Injection, for subcutaneous use

50 mg/0.4 mL

Orencia (available as disposable prefilled syringe)

Bristol-Myers Squibb

87.5 mg/0.7 mL

Orencia (available as disposable prefilled syringe)

Bristol-Myers Squibb

125 mg/mL

Orencia (available as disposable prefilled syringe and prefilled auto-injector [ClickJect])

Bristol-Myers Squibb

AHFS DI Essentials™. © Copyright 2021, Selected Revisions February 1, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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