Last reviewed 2026-04-23 · How we verify

TAK-788

TAK-788 is a selective inhibitor of epidermal growth factor receptor (EGFR) exon 20 insertion mutations.

TAK-788 is a selective inhibitor of epidermal growth factor receptor (EGFR) exon 20 insertion mutations. Used for Non-small cell lung cancer with EGFR exon 20 insertion mutations.

At a glance

Mechanism of action

TAK-788 targets a specific class of EGFR mutations (exon 20 insertions) that confer resistance to standard EGFR tyrosine kinase inhibitors. By selectively inhibiting this mutant form of EGFR, the drug aims to block aberrant signaling that drives cancer cell proliferation in patients with these rare EGFR variants. This mechanism addresses an unmet need in non-small cell lung cancer patients who lack effective treatment options for exon 20 insertion mutations.

Approved indications

• Non-small cell lung cancer with EGFR exon 20 insertion mutations

Common side effects

• Diarrhea
• Rash
• Nausea
• Vomiting

Key clinical trials

• A Study of TAK-788 in Adults With Non-Small Cell Lung Cancer (PHASE1, PHASE2)
• Drug-Drug Interaction Study of TAK-788 and Midazolam in Participants With Advanced Non-small Cell Lung Cancer (NSCLC) (PHASE1)
• A Study of Mobocertinib in Japanese Adults With Non-Small Cell Lung Cancer (PHASE1)
• TAK-788 as First-Line Treatment Versus Platinum-Based Chemotherapy for Non-Small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion Mutations (PHASE3)
• A Study to Assess Absolute Bioavailability (ABA) of Mobocertinib (TAK-788) and to Characterize Mass Balance, Pharmacokinetics (PK), Metabolism, and Excretion of Carbon-14 ([14C])-Mobocertinib in Male Healthy Participants (PHASE1)
• A Study of Mobocertinib Capsules in People With Severe Kidney Problems and People With Healthy Kidneys (PHASE1)
• A Study to Evaluate Pharmacokinetics (PK) and Safety of Oral Mobocertinib in Participants With Moderate or Severe Hepatic Impairment (HI) and Normal Hepatic Function (PHASE1)
• A Study to Evaluate the Effect of High-Fat Meal on TAK-788 Pharmacokinetics (PK) in Healthy Adult Participants (PHASE1)

Primary sources

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