Upajak Prescribe Information

Upadacitinib INN

COMPOSITION

UPAJAK tablet: Each extended-release film-coated tablet contains Upadacitinib INN 15 mg.

PHARMACOLOGY

Upadacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function.

Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression.

Upadacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.

INDICATION

Upajak is a Janus kinase (JAK) inhibitor indicated for:

  • Treatment of adults with moderate to severe active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

     

  • Treatment of adults and pediatric patients 2 years and older with active psoriatic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

     

  • Treatment of adults and pediatric patients 12 years and older with refractory, moderate to severe atopic dermatitis whose disease is not adequately controlled with other systemic drug products, including biologics, or when use of those therapies are inadvisable.

     

  • Treatment of adults with moderately to severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers.

     

  • Treatment of adults with moderately to severely active Crohn’s disease who have had an inadequate response or intolerance to one or more TNF blockers.

     

  • Treatment of adults with active ankylosing spondylitis who have had an inadequate response or intolerance to one or more TNF blockers.

     

  • Treatment of adults with active non-radiographic axial spondyloarthritis with objective signs of inflammation who have had an inadequate response or intolerance to TNF blocker therapy.

     

  • Treatment of patients 2 years of age and older with active polyarticular juvenile idiopathic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

     

Limitation of Use

Not recommended for use in combination with other JAK inhibitors, biological immunomodulators, or with other potent immunosuppressants.

Preliminary tests prior prescribing Upadacitinib

  • Active and latent tuberculosis (TB) infection evaluation — If positive, treat for TB prior to Upadacitinib use.

     

  • Viral hepatitis screening in accordance with clinical guidelines — Upadacitinib initiation is not recommended in patients with active hepatitis B or hepatitis C.

     

  • A complete blood count — Upadacitinib initiation is not recommended in patients with:

     

    • Absolute lymphocyte count < 500 cells/mm³

       

    • Absolute neutrophil count < 1000 cells/mm³

       

    • Hemoglobin < 8 g/dL

       

  • Baseline hepatic function — Upadacitinib initiation is not recommended for patients with severe hepatic impairment (Child-Pugh C).

     

  • Pregnancy status: Verify pregnancy status of females of reproductive potential prior to starting treatment.

DOSAGE AND ADMINISTRATION

Rheumatoid Arthritis

15 mg once daily.

Psoriatic Arthritis (Adults 18 years & older)

15 mg once daily.

Atopic Dermatitis

  • Age 12–65 kg (weighing at least 40 kg): initiate with 15 mg once daily.

     

  • If inadequate response: may increase to 30 mg once daily.

     

  • Discontinue if adequate response is not achieved with the 30 mg dose.

Adults 65 years & older

15 mg once daily.

Ulcerative Colitis (Adults)

  • Induction: 45 mg once daily for 8 weeks.

     

  • Maintenance: 15 mg once daily.

     

    • A dosage of 30 mg once daily may be considered for patients with refractory, severe or extensive disease.

       

    • Discontinue if no adequate therapeutic response with the 30 mg dose.

Crohn’s Disease (Adults)

  • Induction: 45 mg once daily for 12 weeks.

     

  • Maintenance: 15 mg once daily.

     

    • A dosage of 30 mg once daily may be considered for refractory, severe or extensive disease.

       

    • Discontinue if no adequate therapeutic response with the 30 mg dose.

Ankylosing Spondylitis

15 mg once daily.

Non-radiographic Axial Spondyloarthritis

15 mg once daily.

Polyarticular Juvenile Idiopathic Arthritis (≥30 kg)

15 mg once daily.

CONTRAINDICATION

Known hypersensitivity to upadacitinib or any of the excipients in upadacitinib.

WARNINGS AND PRECAUTION

Serious Infections

Avoid use in patients with active, serious infections, including localized infections.

Hypersensitivity

Serious hypersensitivity reactions (e.g., anaphylaxis) have been reported. Discontinue if such a reaction occurs.

Gastrointestinal (GI) Perforations

Monitor at-risk patients; evaluate promptly if symptoms present.

Laboratory Abnormalities

Monitoring recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids.

Embryo-Fetal Toxicity

May cause fetal harm. Advise females of reproductive potential of risk to fetus; use effective contraception.

Vaccinations

Avoid live vaccines.

Medication Residue in Stool

Observed in stool or ostomy output in patients with shortened GI transit. Monitor and consider alternative treatment if response is inadequate.

SIDE EFFECTS

Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, non-radiographic axial spondyloarthritis

Adverse reactions (≥1%):

  • Upper respiratory tract infections
  • Herpes zoster
  • Herpes simplex
  • Bronchitis
  • Nausea
  • Cough
  • Pyrexia
  • Acne
  • Headache

Atopic Dermatitis

Adverse reactions (≥1%):

  • Upper respiratory tract infections
  • Acne
  • Herpes simplex
  • Headache
  • Blood creatine phosphokinase increased
  • Cough
  • Hypersensitivity
  • Folliculitis
  • Nausea
  • Abdominal pain
  • Pyrexia
  • Increased weight
  • Herpes zoster
  • Influenza
  • Fatigue
  • Neutropenia
  • Myalgia
  • Influenza-like illness

Ulcerative Colitis

Adverse reactions (≥5%) during induction or maintenance:

  • Upper respiratory tract infections
  • Increased blood creatine phosphokinase
  • Acne
  • Neutropenia
  • Elevated liver enzymes
  • Rash

Crohn’s Disease

Adverse reactions (≥5%) during induction or maintenance:

  • Upper respiratory tract infections
  • Anemia
  • Pyrexia
  • Acne
  • Herpes zoster
  • Headache

USE IN SPECIFIC POPULATIONS

Pregnancy

Animal studies show potential fetal risks including skeletal and cardiovascular malformations, post-implantation loss, decreased fetal body weights. Human data is limited; all pregnancies carry risk. Increased disease activity may worsen pregnancy outcomes.

Lactation

Advise not to breastfeed.

Pediatric Use

No data for children <2 years.

Hepatic Impairment

Not recommended for severe hepatic impairment.

Renal Impairment

  • No dosage adjustment for RA, psoriatic arthritis, ankylosing spondylitis, non-radiographic axial spondyloarthritis, or polyarticular juvenile idiopathic arthritis with mild–severe renal impairment.
  • For atopic dermatitis: max dose 15 mg daily with severe renal impairment.
  • For ulcerative colitis or Crohn’s disease with severe renal impairment:
    • Induction: 30 mg once daily
    • Maintenance: 15 mg once daily
  • Not recommended in end-stage renal disease.

OVERDOSE

Monitor for signs/symptoms of adverse reactions. Provide appropriate treatment.

DRUG INTERACTIONS

  • Exposure increased with strong CYP3A4 inhibitors (e.g., ketoconazole).
  • Use caution with strong CYP3A4 inhibitors in chronic treatment.
  • Exposure decreased with strong CYP3A4 inducers (e.g., rifampin) — leading to reduced efficacy.
  • Not recommended with strong CYP3A4 inducers.

PHARMACEUTICAL INFORMATION

Storage Condition

Store below 30°C, in a cool dry place. Keep away from light and out of reach of children.

How Supplied

UPAJAK tablet:
 Each HDPE container contains 30 tablets (each tablet contains 15 mg Upadacitinib), a silica gel desiccant and polyester coil with child-resistant closure.

Manufactured by

Everest Pharmaceuticals Ltd.
 BSCIC I/A, Kanchar, Narayanganj, Bangladesh
 www.everestpharmabd.com

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