Selpercatinib
| Evidence Level: L5 | Predicted Indications: 10 |
Table of Contents
Selpercatinib: From RET-Driven Cancers to Pulmonary Hypertension
One-Sentence Summary
Selpercatinib is a selective RET kinase inhibitor, marketed in Singapore as TANSTRIVE capsules. The TxGNN model predicts it may be effective for pulmonary hypertension, but this is a computational prediction only. There are 0 clinical trials and 3 publications compiled, and none of the publications address pulmonary hypertension.
Quick Overview
| Item | Content |
|---|---|
| Original Indication | Not available in the Singapore licence records |
| Predicted New Indication | Pulmonary hypertension |
| TxGNN Prediction Score | 99.18% |
| Evidence Level | L5 |
| Singapore Market Status | ✓ Marketed |
| Number of Registrations | 2 |
| Recommended Decision | Hold |
Why is This Prediction Reasonable?
Currently, detailed mechanism of action data is not available in the data compiled for this report. Selpercatinib is known to be a selective RET kinase inhibitor, and the publications retrieved concern RET-driven cancers (RET fusion-positive non-small-cell lung cancer and RET-mutated medullary thyroid carcinoma).
The analysis found no established mechanistic link between RET inhibition and pulmonary hypertension. RET signalling has no well-validated role in pulmonary vascular remodelling. The high TxGNN score is a computational output that likely reflects knowledge-graph proximity. Any plausible link, such as off-target kinase effects on vascular signalling, would be speculative and is not supported by the data.
Other predictions in the same list (for example migraine, idiopathic pulmonary arterial hypertension, and several rare skeletal or skin conditions) are also supported only by model scores, with no clinical evidence. Idiopathic pulmonary arterial hypertension is the closest related entry. Some multi-kinase inhibitors have been studied there, but selpercatinib is highly RET-selective, so extrapolating from that class is weak.
Clinical Trial Evidence
Currently no related clinical trials registered.
Literature Evidence
| PMID | Year | Type | Journal | Key Findings |
|---|---|---|---|---|
| 34178121 | 2021 | Retrospective analysis | Therapeutic Advances in Medical Oncology | Real-world use of selpercatinib in RET fusion-positive NSCLC through an access program. Not related to pulmonary hypertension. |
| 39372206 | 2024 | Pharmacovigilance study | Frontiers in Pharmacology | Compares adverse event profiles of pralsetinib and selpercatinib using FDA adverse event reports. |
| 41918669 | 2026 | Case report | Cureus | Long-term management and targeted therapy of metastatic medullary thyroid carcinoma in MEN 2B with RET M918T mutation. |
Singapore Market Information
| Authorization Number | Product Name | Dosage Form | Approved Indication |
|---|---|---|---|
| SIN16991P | TANSTRIVE HARD CAPSULES 80MG | Capsule | Not stated in the records |
| SIN16990P | TANSTRIVE HARD CAPSULES 40MG | Capsule | Not stated in the records |
Cytotoxicity
| Item | Content |
|---|---|
| Cytotoxicity Classification | Targeted therapy (selective RET kinase inhibitor) |
| Myelosuppression Risk | Please refer to the package insert warnings and precautions |
| Emetogenicity Classification | Please refer to the package insert warnings and precautions |
| Monitoring Items | Please refer to the package insert warnings and precautions |
| Handling Protection | Please refer to the package insert warnings and precautions |
Safety Considerations
- Drug Interactions: The interaction screening returned 100 interacting drugs in total. Examples flagged as Major include:
- Acid-suppressing agents: famotidine, ranitidine, cimetidine, omeprazole, rabeprazole, dexlansoprazole
- Aprepitant
- Clarithromycin
- Dexamethasone
- Magnesium oxide
Examples flagged as Moderate include hydrocortisone, triamcinolone, betamethasone, budesonide, pioglitazone, saxagliptin, loperamide, bisacodyl, and polyethylene glycol with electrolytes.
For warnings and contraindications, please refer to the package insert, as this information was not available in the data compiled for this report.
Conclusion and Next Steps
Decision: Hold
Rationale: The prediction rests only on a model score (L5). There are no clinical trials, none of the retrieved literature addresses pulmonary hypertension, and no mechanistic link between RET inhibition and pulmonary vascular disease could be identified.
To proceed, the following is needed:
- Mechanism of action data, to allow proper mechanistic-link analysis
- Package insert warnings and contraindications from HSA, which are needed before safety screening
- Preclinical or mechanistic evidence that RET inhibition affects pulmonary vascular remodelling
- Literature or trial evidence specific to pulmonary hypertension
- A review of the major drug interactions, particularly acid-suppressing agents, if any clinical use is considered
Disclaimer
This content is for research purposes only and does not constitute medical advice. Clinical validation is required before any clinical application.