^
3d
New P2 trial • Metastases
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Lenvima (lenvatinib) • adebrelimab (SHR-1316)
3d
LITESPARK-016: Pembrolizumab Plus Lenvatinib in Combination With Belzutifan in Solid Tumors (MK-6482-016) (clinicaltrials.gov)
P2, N=730, Recruiting, Merck Sharp & Dohme LLC | Trial completion date: Aug 2026 --> Mar 2027 | Trial primary completion date: Aug 2026 --> Mar 2027
Trial completion date • Trial primary completion date • Combination therapy
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MSI (Microsatellite instability)
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Keytruda (pembrolizumab) • Lenvima (lenvatinib) • Welireg (belzutifan)
4d
Exploring the Impact of Hepatic Impairment on Pralsetinib Pharmacokinetics. (PubMed, Pharmaceutics)
Results based on the NCI-ODWG classification criteria were comparable; the AUC0-∞ GMR were 1.22 and 0.858, respectively, for subjects with moderate and severe HI per NCI-ODWG versus those with normal hepatic function. These results suggested that moderate and severe hepatic impairment did not have a meaningful impact on the exposure to pralsetinib, thus not warranting a dose adjustment in this population.
PK/PD data • Journal
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RET (Ret Proto-Oncogene)
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RET fusion
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Gavreto (pralsetinib)
5d
Antiproliferative Activity of N-Acylhydrazone Derivative on Hepatocellular Carcinoma Cells Involves Transcriptional Regulation of Genes Required for G2/M Transition. (PubMed, Biomedicines)
Multikinase inhibitors sorafenib (Nexavar®) and lenvatinib (Lenvima®) have been used as first-line drugs with modest therapeutic effects. In addition, LASSBio-2052 significantly reduced CCNB1 and CCND1 expression in HCC cells. Our findings indicate that LASSBio-2052 is a promising prototype for further in vivo studies.
Journal
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CCND1 (Cyclin D1) • KDR (Kinase insert domain receptor) • AURKA (Aurora kinase A) • PLK1 (Polo Like Kinase 1) • AURKB (Aurora Kinase B) • FOXM1 (Forkhead Box M1) • CDK1 (Cyclin-dependent kinase 1) • CCNB1 (Cyclin B1)
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CCND1 expression
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sorafenib • Lenvima (lenvatinib)
5d
Predictive insights into plant-based compounds as fibroblast growth factor receptor 1 inhibitors: a combined molecular docking and dynamics simulation study. (PubMed, J Biomol Struct Dyn)
To gain further insights into the conformational dynamics of Mundulone and the reference FGFR1 inhibitor, Lenvatinib, we conducted time-evolution analyses employing 200 ns molecular dynamics simulations (MDS) and essential dynamics...Overall, the findings indicate that Mundulone exhibits promising binding affinity, specific interactions, and favorable drug profiles, making it a promising lead candidate. Further experimental analysis will be necessary to confirm its effectiveness and safety profiles for therapeutic advancement in the cancer field.Communicated by Ramaswamy H. Sarma.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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Lenvima (lenvatinib)
5d
Comparative analysis of sorafenib and lenvatinib on HepG2 cells and human umbilical vein endothelial cells: Involvement of transforming growth factor-β signaling in their molecular effects. (PubMed, Hepatol Res)
Our findings indicate that both sorafenib and lenvatinib possess anticancer abilities by inducing the cytotoxicity of hepatocellular carcinoma cells. Furthermore, they show opposing effects on TGF-β-induced cell invasion and angiogenesis, thereby enhancing the understanding of the multifaceted functions of molecular targeted drugs in treating hepatocellular carcinoma.
Journal
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TGFBR2 (Transforming Growth Factor Beta Receptor 2) • TGFB1 (Transforming Growth Factor Beta 1)
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sorafenib • Lenvima (lenvatinib)
7d
Clinical Activity of Selpercatinib in RET-mutant Pheochromocytoma. (PubMed, J Clin Endocrinol Metab)
These data support selpercatinib as an effective therapy against RET-mutant pheochromocytoma, adding to the diversity of RET-activated tumor types that may benefit from targeted RET inhibition.
Journal
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RET (Ret Proto-Oncogene)
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RET mutation
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Retevmo (selpercatinib)
7d
Efficacy and predictive factors of transarterial chemoembolization combined with lenvatinib plus programmed cell death protein-1 inhibition for unresectable hepatocellular carcinoma. (PubMed, World J Gastrointest Oncol)
This study showed that TACE/lenvatinib/PD-1 treatment was well tolerated with encouraging efficacy in patients with unresectable HCC. The patients with BCLC B-stage disease with early NLR response (decrease) and early AFP response (decrease > 20%) may achieve better clinical outcomes with this triple therapy.
Journal
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AFP (Alpha-fetoprotein)
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Lenvima (lenvatinib)
7d
New P2 trial • Metastases
|
Tyvyt (sintilimab) • Lenvima (lenvatinib) • capecitabine • oxaliplatin
8d
Genomic and Transcriptomic Landscape of RET Wild-Type Medullary Thyroid Cancer and Potential Use of Mitogen-Activated Protein Kinase-Targeted Therapy. (PubMed, J Am Coll Surg)
We identified molecular alterations and immune-related features that distinguish wtRET from mutRET MTC. While RET mutation drives MTC in the absence of other alterations, we showed that wtRET MTC frequently harbors MAPK pathway mutations. These findings may indicate a potential basis for MAPK-targeted therapy, possibly in combination with oncology immune-oncology agents for selected patients with wtRET MTC.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • TMB (Tumor Mutational Burden) • RET (Ret Proto-Oncogene) • STK11 (Serine/threonine kinase 11) • HRAS (Harvey rat sarcoma viral oncogene homolog) • NF1 (Neurofibromin 1)
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PD-L1 expression • KRAS mutation • TMB-H • BRAF mutation • STK11 mutation • NF1 mutation • RET mutation • VHL mutation • HRAS mutation • RET wild-type
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Retevmo (selpercatinib)
9d
Selpercatinib for treating recurrent mixed medullary and follicular cell-derived thyroid carcinoma: a case report. (PubMed, Surg Case Rep)
We report a rare case of selpercatinib use for MMFCC. Since RET mutations may occur frequently in MMFCC, selpercatinib could be effective in treating MMFCC.
Journal
|
RET (Ret Proto-Oncogene)
|
RET mutation • RET M918T
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Oncomine™ Dx Target Test
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Retevmo (selpercatinib)
11d
HAIC Combined with lenvatinib plus PD-1 versus lenvatinib Plus PD-1 in patients with high-risk advanced HCC: a real-world study. (PubMed, BMC Cancer)
Lenvatinib, HAIC and PD-1 showed safe and promising anti-tumor activity compared with lenvatinib alone for HCC with high-risk features.
Journal • Real-world evidence • Real-world • Metastases
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PD-1 (Programmed cell death 1)
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Lenvima (lenvatinib)
14d
New P2 trial
|
PD-L1 (Programmed death ligand 1)
|
Keytruda (pembrolizumab) • Lenvima (lenvatinib)
14d
Predicting Response to Immunotargeted Therapy in Endometrial Cancer via Tumor Immune Microenvironment: A Multicenter, Observational Study. (PubMed, Int J Mol Sci)
Only one-third of patients with advanced MSS/pMMR endometrial cancer exhibit a lasting response to the combination treatment of Pembrolizumab and Lenvatinib. The sensitivity and specificity of these biomarkers were 85.71% and 70.59%, and 85.71% and 85.71%, respectively. The proportion of CD20+ B lymphocytes and the CD8-to-CD20 lymphocytes ratio in the stroma of endometrial cancer serves as both a prognostic marker of response to immunotargeted therapy and a prognostic factor for progression-free survival in patients.
Observational data • Journal • PD(L)-1 Biomarker
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CD20 (Membrane Spanning 4-Domains A1) • CD8 (cluster of differentiation 8) • CD163 (CD163 Molecule) • FOXP3 (Forkhead Box P3)
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Keytruda (pembrolizumab) • Lenvima (lenvatinib)
14d
Genomic landscape and clinical features of advanced thyroid carcinoma: a national database study in Japan. (PubMed, J Clin Endocrinol Metab)
Genetic abnormalities with treatment options were found in 62.7% of advanced thyroid carcinomas. TP53 abnormality was an independent poor prognostic factor for overall survival in differentiated thyroid carcinoma. The time to treatment failure for lenvatinib was not different based on genetic profile.
Journal • Metastases
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BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • TP53 (Tumor protein P53) • RET (Ret Proto-Oncogene) • NTRK (Neurotrophic receptor tyrosine kinase)
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TP53 mutation • BRAF V600E • BRAF V600 • RET fusion • ALK fusion • RAS mutation • NTRK fusion
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Lenvima (lenvatinib)
15d
Trial completion date • Trial primary completion date • Metastases
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Keytruda (pembrolizumab) • Lenvima (lenvatinib)
16d
Lenvatinib and Everolimus in Renal Cell Carcinoma (RCC) (clinicaltrials.gov)
P1, N=11, Active, not recruiting, Yousef Zakharia | Trial completion date: Sep 2024 --> Jun 2028
Trial completion date • Metastases
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everolimus • Lenvima (lenvatinib)
20d
Recent advances in tyrosine kinase inhibitors VEGFR 1-3 for the treatment of advanced metastatic melanoma. (PubMed, Expert Opin Pharmacother)
On the contrary, some patients with mucosal, acral or KIT-mutant melanoma may benefit from TKI-based therapies. Further studies focused on biomarker discovery and randomized trials are necessary to better understand the role of VEGFR1-3 as a therapeutic target in melanoma.
Review • Journal • PD(L)-1 Biomarker • IO biomarker • Metastases
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KIT (KIT proto-oncogene, receptor tyrosine kinase) • FLT1 (Fms-related tyrosine kinase 1)
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KIT mutation
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Lenvima (lenvatinib) • AiTan (rivoceranib) • Inlyta (axitinib)
20d
New P2 trial • Metastases
|
cisplatin • Lenvima (lenvatinib) • Loqtorzi (toripalimab-tpzi) • oxaliplatin
20d
New P2 trial
|
Lenvima (lenvatinib) • Kaitanni (cadonilimab)
21d
New P1 trial
23d
AMBER: AMG510 (Sotorasib) Plus Lenvatinib as Second-line Treatment in Patients With KRASG12C Mutant, Metastatic NSCLC (clinicaltrials.gov)
P2, N=0, Withdrawn, ETOP IBCSG Partners Foundation | N=47 --> 0 | Not yet recruiting --> Withdrawn
Enrollment change • Trial withdrawal • Metastases
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation • KRAS G12C • KRAS G12
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Lenvima (lenvatinib) • Lumakras (sotorasib)
23d
LENVABLA: Neoadjuvant and Adjuvant Lenvatinib in HCC Patients Treated by Percutaneous Ablative (clinicaltrials.gov)
P2, N=32, Active, not recruiting, Assistance Publique - Hôpitaux de Paris | Recruiting --> Active, not recruiting | N=50 --> 32 | Trial completion date: Feb 2025 --> Oct 2026 | Trial primary completion date: Apr 2024 --> Jul 2025
Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
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AFP (Alpha-fetoprotein) • FLT4 (Fms-related tyrosine kinase 4) • VEGFC (Vascular Endothelial Growth Factor C)
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Lenvima (lenvatinib)
23d
Determination of Pralsetinib in Human Plasma and Cerebrospinal Fluid for Therapeutic Drug Monitoring by Ultra-performance Liquid Chromatography-Tandem Mass Spectrometry (UPLC-MS/MS). (PubMed, Anticancer Agents Med Chem)
We have developed a quick and effective method for concentration detection in both plasma and CSF, and it can be applied for drug monitoring in clinical practice. The method can also provide a reference for further optimization.
Journal
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RET (Ret Proto-Oncogene)
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Xalkori (crizotinib) • Tagrisso (osimertinib) • Gilotrif (afatinib) • Gavreto (pralsetinib)
24d
New P1 trial
|
SY-5007
28d
Trial completion
|
RET (Ret Proto-Oncogene)
|
RET fusion • RET mutation • RET rearrangement
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Gavreto (pralsetinib)
1m
Nuclear KRT19 is a transcriptional co-repressor promoting histone deacetylation and liver tumorigenesis. (PubMed, Hepatology)
Our data show that nuclear KRT19 acts as a transcriptional co-repressor through promoting the deacetylase activity of the CoREST complex, resulting in dedifferentiation of liver cancer. These findings reveal a previously unrecognized function of KRT19 in directly shaping the epigenetic landscape in cancer.
Journal
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HDAC1 (Histone Deacetylase 1) • KRT19 (Keratin 19) • HNF1A (HNF1 Homeobox A)
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Lenvima (lenvatinib)
1m
Surgical Intervention After Lenvatinib Treatment in Patients With Advanced Hepatocellular Carcinoma. (PubMed, Anticancer Res)
Surgical intervention after lenvatinib treatment for advanced HCC was associated with longer PFS. Patients exhibiting decreased AFP levels or maintaining AFP levels within the normal limit may be suitable candidates for surgical intervention after lenvatinib treatment for advanced HCC.
Journal • Metastases
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AFP (Alpha-fetoprotein)
|
AFP elevation
|
Lenvima (lenvatinib)
1m
Cadonilimab and Lenvatinib for Conversion Therapy in Unresectable Hepatocellular Carcinoma (clinicaltrials.gov)
P2, N=30, Recruiting, Peking Union Medical College Hospital | Not yet recruiting --> Recruiting
Enrollment open
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Lenvima (lenvatinib) • Kaitanni (cadonilimab)
1m
Repression of LSD1/KDM1A activity improves the response of liver cancer cells to the lenvatinib. (PubMed, Discov Oncol)
Pulrodemstat synergized with Lenvatinib based on suppression of PI3K-AKT signaling and activation of apoptotic signaling.
Journal
|
CASP3 (Caspase 3)
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Lenvima (lenvatinib) • pulrodemstat (CC-90011)
1m
New P1 trial
|
SY-5007 • itraconazole • rifampicin
1m
New trial • Real-world evidence • Real-world
|
5-fluorouracil • Tyvyt (sintilimab) • Lenvima (lenvatinib) • Loqtorzi (toripalimab-tpzi) • AiRuiKa (camrelizumab) • Tevimbra (tislelizumab) • oxaliplatin
1m
A Study of LOXO-260 in Cancer Patients With a Change in a Particular Gene (RET) That Has Not Responded to Treatment (clinicaltrials.gov)
P1, N=110, Active, not recruiting, Eli Lilly and Company | Recruiting --> Active, not recruiting | Trial completion date: Apr 2026 --> Jun 2025 | Trial primary completion date: Apr 2026 --> Jun 2025
Enrollment closed • Trial completion date • Trial primary completion date
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RET (Ret Proto-Oncogene)
|
RET fusion • RET mutation
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LOXO-260
1m
Population pharmacokinetic-pharmacodynamic modeling of serum biomarkers as predictors of tumor dynamics following lenvatinib treatment in patients with radioiodine-refractory differentiated thyroid cancer (RR-DTC). (PubMed, CPT Pharmacometrics Syst Pharmacol)
Longitudinal tumor measurements over time were reasonably well defined by a tumor growth inhibition Emax model, which in addition to lenvatinib exposure, included model-predicted relative changes from baseline over time for Tie-2 and Ang-2 as having significant association with tumor response. The developed PK/PD models pave the way for dose optimization and potential prediction of clinical response.
PK/PD data • Journal
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PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • FGF23 (Fibroblast Growth Factor 23)
|
Lenvima (lenvatinib)
1m
Phase II Study of Pembrolizumab and Lenvatinib in Advanced Well-differentiated Neuroendocrine Tumors (clinicaltrials.gov)
P2, N=20, Active, not recruiting, H. Lee Moffitt Cancer Center and Research Institute | Trial completion date: Jan 2024 --> Jul 2024
Trial completion date • Metastases
|
Keytruda (pembrolizumab) • Lenvima (lenvatinib)
1m
A Study of Lenvatinib in Combination With Pembrolizumab in Korean Patients (clinicaltrials.gov)
P=N/A, N=135, Completed, Eisai Korea Inc. | Recruiting --> Completed | N=98 --> 135
Trial completion • Enrollment change • Combination therapy
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Keytruda (pembrolizumab) • Lenvima (lenvatinib)
1m
New P1 trial
|
sorafenib • Lenvima (lenvatinib)
1m
New P1 trial
|
SY-5007
1m
The Study of KN046 in Combination With Lenvatinib in Advanced Hepatocellular Carcinoma (clinicaltrials.gov)
P2, N=55, Completed, Peking University Cancer Hospital & Institute | Recruiting --> Completed | Trial completion date: May 2023 --> Mar 2024
Trial completion • Trial completion date • Combination therapy • Metastases
|
Lenvima (lenvatinib) • erfonrilimab (KN046)
1m
Nivolumab Plus Lenvatinib Against Anaplastic Thyroid Cancer (NAVIGATION) (clinicaltrials.gov)
P2, N=51, Active, not recruiting, National Cancer Center Hospital East | Recruiting --> Active, not recruiting
Enrollment closed
|
Opdivo (nivolumab) • Lenvima (lenvatinib)
1m
Using Chronobiology to Improve Lenvatinib Efficacy (clinicaltrials.gov)
P1, N=10, Recruiting, Hadassah Medical Organization
New P1 trial
|
Lenvima (lenvatinib)
1m
Phase II study of pembrolizumab and lenvatinib in advanced well-differentiated neuroendocrine tumors. (PubMed, ESMO Open)
The combination of pembrolizumab and lenvatinib did not show sufficient response in patients with NETs to warrant continued enrollment on trial.
P2 data • Journal • Metastases
|
FGFR (Fibroblast Growth Factor Receptor)
|
Keytruda (pembrolizumab) • Lenvima (lenvatinib)