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CAMBRITAXESTAT
Generic Name: CAMBRITAXESTAT
ABSTRACT -
Cambritaxestat (GLPG1690) is an oral, potent autotaxin (ATX) inhibitor developed by Galapagos for idiopathic pulmonary fibrosis (IPF). Autotaxin converts lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA), a pro-fibrotic mediator. By inhibiting ATX, cambritaxestat reduces LPA levels in the lung, potentially slowing fibrotic progression. However, Phase III trials (ISABELA 1 and 2) were terminated early due to excess mortality in the treatment arm.
DOSAGE -
Oral capsule; 200 mg once daily was studied in Phase III; development halted following IDMC safety review.
SIDE EFFECTS -
- Increased mortality observed in Phase III (reason for trial halt)
- Nausea
- Diarrhoea
- Respiratory infections
- Elevated creatine phosphokinase
ALLERGIC REACTIONS -
These symptoms may indicate an allergic reaction and require immediate medical attention.
- Skin rash
- Hypersensitivity reactions
- Urticaria
- Angioedema (rare)
DRUG INTERACTIONS-
- Interaction with statins (creatine phosphokinase monitoring)
- CYP3A4 interactions possible
- Avoid in combination with immunosuppressants in IPF
PREAUTONS–
- Development suspended — not for clinical use outside ongoing safety review
- Survival monitoring in any future trial would be mandatory
- No approved indication as of 2024
WARNINGS –
- Phase III terminated due to excess deaths in treatment arm versus placebo
- Drug is NOT approved — use outside clinical trials contraindicated
- Do not use as IPF therapy pending full safety evaluation
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