Initial US Approval

  • 20221

Indications

  • Adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with a rearranged during transfection (RET) gene fusion, as detected by an FDA-approved test.1
  • Adult and pediatric patients 2 years of age and older with advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an FDA-approved test, who require systemic therapy.1
  • Adult and pediatric patients 2 years of age and older with advanced or metastatic thyroid cancer with a RET gene fusion, as detected by an FDA-approved test, who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate).1
  • Adult and pediatric patients 2 years of age and older with locally advanced or metastatic solid tumors with a RET gene fusion, as detected by an FDA-approved test, that have progressed on or following prior systemic treatment or who have no satisfactory alternative treatment options. This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s).1

Recommended Dose/Route

  • Less than 50 kg: 160 mg orally, twice daily, with or without food1
  • 50 kg or greater: 120 mg orally, twice daily, with or without food1
Dose Reductions for Adverse Reactions with Selpercatinib

Dose Reductions for Adverse Reactions with Selpercatinib

Pivotal Study

  • LIBRETTO-001 (NCT03157128)1,2
  • Key Inclusion Criteria: Eligible patients were aged 18 years or older with RET-altered cancers, with disease progression on or after previous systemic therapies or no satisfactory therapeutic options, and an Eastern Cooperative Oncology Group (ECOG) performance status score of 0-23.1,2
  • Treatment: Selpercatinib, 160 mg orally, twice daily until disease progression or unacceptable toxicity.1,2
Selpercatinib: Efficacy Data

Selpercatinib: Efficacy Data

Safety

  • Common Adverse Reactions (≥20%): The most frequently reported any grade AEs were edema (49%), diarrhea (47%), fatigue (46%), dry mouth (43%), hypertension (41%), abdominal pain (34%), constipation (33%), rash (33%), nausea (31%), headache (28%), cough (24%), vomiting (22%), dyspnea (22%), hemorrhage (22%), arthralgia (21%), and prolonged QT interval (21%).1,2
  • Common Laboratory Abnormalities (≥30%): The most frequently reported laboratory abnormalities were increased AST (59%), decreased calcium (59%), increased ALT (56%), decreased albumin (56%), increased glucose (53%), decreased lymphocytes (52%), increased creatine (47%), decreased sodium (42%), increased alkaline phosphatase (40%), decreased platelets (37%), increased total cholesterol (45%), increased potassium (34%), decreased glucose (34%), decreased magnesium (33%), and increased bilirubin (30%).1,2
  • Dosage Interruption Due to Adverse Events (AEs): 64%1
  • Dosage Reductions Due to AEs: 41%1
  • Permanent Discontinuation Due to AEs: 8%1

References

  1. RETEVMO (selpercatinib). Prescribing information. Eli Lilly and Company; 2022. https://pi.lilly.com/us/retevmo-uspi.pdf?s=pi
  2. Subbiah V, Wolf J, Konda B, et al. Tumour-agnostic efficacy and safety of selpercatinib in patients with RET fusion-positive solid tumours other than lung or thyroid tumours (LIBRETTO-001): a phase 1/2, open-label, basket trial. Lancet Oncol. 2022;23(10):1261-1273. doi:10.1016/S1470-2045(22)00541-1
  3. Duke ES, Bradford D, Marcovitz M, et al. FDA Approval Summary: Selpercatinib for the Treatment of Advanced RET Fusion-Positive Solid Tumors. Clinical Cancer Research. 2023;29(18):3573-3578. doi:10.1158/1078-0432.CCR-23-0459
  4. Nardo M, Gouda MA, Nelson BE, et al. Strategies for mitigating adverse events related to selective RET inhibitors in patients with RET-altered cancers. Cell Rep Med. 2023;4(12):101332. doi:10.1016/j.xcrm.2023.101332