ArticleTargeted oncology2026
First-in-Human Phase I Study of KPT-9274, a First-in-Class Dual Inhibitor of PAK4 and NAMPT, in Patients with Advanced Solid Malignancies.
Article in Targeted oncology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02702492 (A Phase 1 Open-Label Study of the Safety, Tolerability and Efficacy of KPT-9274, a Dual Inhibitor of PAK4 and NAMPT, in Patients With Advanced Solid Malignancies or Non-Hodgkin's Lymphoma), which is not on this map. Cited by 18 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
A Phase 1 Open-Label Study of the Safety, Tolerability and Efficacy of KPT-9274, a Dual Inhibitor of PAK4 and NAMPT, in Patients With Advanced Solid Malignancies or Non-Hodgkin's Lymphoma
Who cites it
18 citing papers in PubMed.
- Comment on: "First-in-Human Phase I Study of KPT-9274, a First-in-Class Dual Inhibitor of PAK4 and NAMPT, in Patients with Advanced Solid Malignancies".Targeted oncology · 2026Article
- Computational Identification of New Dual PAK4 and NAMPT Inhibitors.International journal of molecular sciences · 2026Article
- Nuclear-Cytoplasmic Axis in Cancer: From Protein Mislocalization to Anticancer Drug Resistance.Oncology research · 2026Review
- Targeting NAD+ Metabolism Vulnerability in FH-Deficient Hereditary Leiomyomatosis and Renal Cell Carcinoma with the Novel NAMPT Inhibitor OT-82.Molecular cancer therapeutics · 2025Article
- Visfatin Promotes Renal Cell Carcinoma Progression: Evidence from Clinical Samples and Cell Line Models.Journal of kidney cancer and VHL · 2025Article
- Accelerating CAR-T Cell Therapies with Small-Molecule Inhibitors.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy · 2025Review
- Mechanisms of resistance to NAMPT inhibitors in cancer.Cancer drug resistance (Alhambra, Calif.) · 2025Review
- Repurposing NAMPT Inhibitors for Germinal Center B Cell-Like Diffuse Large B-Cell Lymphoma.Blood cancer discovery · 2024Article
- Biological Functions and Therapeutic Potential of NADCancers · 2024Review
- Dual-inhibition of NAMPT and PAK4 induces anti-tumor effects in 3D-spheroids model of platinum-resistant ovarian cancer.Cancer gene therapy · 2024Article
- Channeling Nicotinamide Phosphoribosyltransferase (NAMPT) to Address Life and Death.Journal of medicinal chemistry · 2024Review
- Anticancer Activities of Novel Nicotinamide Phosphoribosyltransferase Inhibitors in Hematological Malignancies.Molecules (Basel, Switzerland) · 2023Article
- Clinical development of metabolic inhibitors for oncology.The Journal of clinical investigation · 2022Review
- PAK4 and NAMPT as Novel Therapeutic Targets in Diffuse Large B-Cell Lymphoma, Follicular Lymphoma, and Mantle Cell Lymphoma.Cancers · 2021Article
- Anti-tumor NAMPT inhibitor, KPT-9274, mediates gender-dependent murine anemia and nephrotoxicity by regulating SIRT3-mediated SOD deacetylation.Journal of hematology & oncology · 2021Article
- p21-activated kinases as viable therapeutic targets for the treatment of high-risk Ewing sarcoma.Oncogene · 2021Article
- Anti-Cancer Activity of PAK4/NAMPT Inhibitor and Programmed Cell Death Protein-1 Antibody in Kidney Cancer.Kidney360 · 2020Article
- Rho GTPase effectors and NAD metabolism in cancer immune suppression.Expert opinion on therapeutic targets · 2018Review
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Authors and funding
12 authors.
Funding
Abstract
backgroundKPT-9274, a potentially first-in-class, dual NAMPT/PAK4 inhibitor, has shown single-agent anticancer activity in hematologic and solid tumor cell lines and xenografts. KPT-9274 has shown anti-tumor activity in combination with nivolumab in nonclinical models.
objectiveKCP-9274-901 was a first-in-human, multi-center, open-label clinical study to assess preliminary safety, tolerability, and efficacy of KPT-9274 in patients with advanced solid tumors. PATIENTS AND
methodsThis study was conducted in three parts. A two-part (A, B) dose escalation phase to determine the recommended phase II dose and maximum tolerated dose (MTD) of KPT-9274 alone and with niacin. Part 3 (C) was a dose-finding and expansion phase in patients with melanoma treated with KPT-9274 plus nivolumab.
resultsA total of 60 patients were enrolled (part A and B n = 50; part C n = 10). Three dose-limiting toxicities (DLTs) were observed in the 40-mg (n = 1) and 80-mg plus niacin (n = 2) cohorts. MTD was not reached in parts A and B and was 60 mg plus nivolumab in part C. The most frequently reported TEAEs (≥30%) were anemia (82.6%), arthralgia (52.2%), and fatigue (43.5%). Patient enrollment was halted prematurely due to a lack of observable efficacy in all parts of the study.
conclusionsThe MTD of KPT-9274 was not reached in a dose escalation study conducted in patients with advanced solid tumors. Clinical activity was not observed at study doses in combination with niacin or nivolumab. Further investigation into potential therapeutic areas where KPT-9274 may serve as a targeted agent is warranted. TRIAL REGISTRY: Clinical trial registration: www. CLINICALTRIALS: gov , NCT02702492.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.