^
10h
New P2 trial • Metastases
|
Tyvyt (sintilimab) • Lenvima (lenvatinib) • capecitabine • oxaliplatin
13h
CDCA5-EEF1A1 interaction promotes progression of clear cell renal cell carcinoma by regulating mTOR signaling. (PubMed, Cancer Cell Int)
Taken together, our results demonstrate the significant role of CDCA5 in ccRCC progression. The findings may provide insights for the development of new treatment strategies targeting CDCA5 for ccRCC patients.
Journal
|
EEF1A1 (Eukaryotic Translation Elongation Factor 1 Alpha 1)
|
Sutent (sunitinib)
22h
Discovery of a Novel Orally Bioavailable FLT3-PROTAC Degrader for Efficient Treatment of Acute Myeloid Leukemia and Overcoming Resistance of FLT3 Inhibitors. (PubMed, J Med Chem)
Most importantly, A20 exerted significantly improved antiproliferative activity against drug-resistant AML cells compared to existing FLT3 inhibitors. These findings suggested that A20 could serve as a promising drug candidate for relapsed or refractory AML.
Journal
|
FLT3 (Fms-related tyrosine kinase 3) • CD33 (CD33 Molecule) • PTPRC (Protein Tyrosine Phosphatase Receptor Type C)
|
FLT3-ITD mutation
2d
Neuropilin-1-Targeted Nanomedicine for Spatiotemporal Tumor Suppression through Photodynamic Vascular Damage and Antiangiogenesis. (PubMed, ACS Appl Mater Interfaces)
In brief, FPPT@Axi is prepared by utilizing an NRP-1-targeting chimeric peptide (Fmoc-K(PpIX)-PEG8-TKPRR) to encapsulate the antiangiogenic drug Axitinib (Axi)...Consequently, FPPT@Axi spatiotemporally restrains the tumor growth through blocking angiogenesis, destroying tumor vessels, and inducing tumor apoptosis. Such an NRP-1-mediated targeting codelivery system sheds light on constructing an appealing candidate with translational potential by using clinically approved PDT and chemotherapy.
Journal
|
NRP1 (Neuropilin 1)
|
Inlyta (axitinib)
3d
Surufatinib combined with photodynamic therapy induces ferroptosis to inhibit cholangiocarcinoma in vitro and in tumor models. (PubMed, Front Pharmacol)
SUR combined with PDT can significantly enhance the inhibitory effect on CCA, and can be alleviated by two ferroptosis inhibitors (Ferrostatin-1, Deferoxamine). In conclusion, SUR combined with PDT exerted an anti-CCA effect by inducing ferroptosis. Combination therapy provides a new idea for the clinical treatment of CCA.
Preclinical • Journal
|
GPX4 (Glutathione Peroxidase 4) • ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4)
|
Sulanda (surufatinib)
3d
KB-LANRA- 1001: A Study to Evaluate Lanraplenib (LANRA) in Combination With Gilteritinib in Participants With FLT3-mutated Relapsed or Refractory Acute Myeloid Leukemia (AML) (clinicaltrials.gov)
P1/2, N=24, Terminated, Kronos Bio | Trial completion date: Oct 2024 --> Apr 2024 | Active, not recruiting --> Terminated; Sponsor decision
Trial completion date • Trial termination • Combination therapy
|
FLT3 (Fms-related tyrosine kinase 3)
|
FLT3 mutation
|
Xospata (gilteritinib) • lanraplenib (GS-9876)
4d
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
|
PD-1 (Programmed cell death 1)
|
Lenvima (lenvatinib)
5d
Multi-omics and immunogenomics analysis revealed PFKFB3 as a targetable hallmark and mediates sunitinib resistance in papillary renal cell carcinoma: in silico study with laboratory verification. (PubMed, Eur J Med Res)
Glycolysis-Immune Risk Signature is closely associated with pRCC prognosis, progression, immune infiltration, and therapeutic response. PFKFB3 may serve as a pivotal glycolysis regulator and mediates Sunitinib resistance in pRCC patients.
Journal
|
PFKFB3 (6-Phosphofructo-2-Kinase/Fructose-2,6-Biphosphatase 3)
|
Sutent (sunitinib)
6d
Pharmacological inhibition of RAS overcomes FLT3 inhibitor resistance in FLT3-ITD+ AML through AP-1 and RUNX1. (PubMed, iScience)
However, cytokine-mediated drug resistance can be overcome by a pan-RAS inhibitor. We show that cytokines instruct AML growth via the transcriptional regulators AP-1 and RUNX1 and that pan-RAS drugs bypass this barrier.
Journal
|
FLT3 (Fms-related tyrosine kinase 3) • RUNX1 (RUNX Family Transcription Factor 1)
6d
Multicenter Trial of ESK981 in Patients With Select Solid Tumors (clinicaltrials.gov)
P2, N=66, Recruiting, University of Michigan Rogel Cancer Center | Not yet recruiting --> Recruiting
Enrollment open
|
SYP (Synaptophysin) • CHGA (Chromogranin A)
|
ESK981
6d
New P2 trial • Metastases
|
Sulanda (surufatinib) • adebrelimab (SHR-1316)
8d
New P2 trial
|
PD-L1 (Programmed death ligand 1)
|
Keytruda (pembrolizumab) • Lenvima (lenvatinib)
8d
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
|
CD20 (Membrane Spanning 4-Domains A1) • CD8 (cluster of differentiation 8) • CD163 (CD163 Molecule) • FOXP3 (Forkhead Box P3)
|
Keytruda (pembrolizumab) • Lenvima (lenvatinib)
8d
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
|
BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • TP53 (Tumor protein P53) • RET (Ret Proto-Oncogene) • NTRK (Neurotrophic receptor tyrosine kinase)
|
TP53 mutation • BRAF V600E • BRAF V600 • RET fusion • ALK fusion • RAS mutation • NTRK fusion
|
Lenvima (lenvatinib)
8d
AG-73305 Single Ascending Dose Cohort Study in DME (clinicaltrials.gov)
P2, N=25, Active, not recruiting, Allgenesis Biotherapeutics Inc. | Recruiting --> Active, not recruiting | Phase classification: P2a --> P2
Enrollment closed • Phase classification
8d
Trial completion date • Trial primary completion date • Metastases
|
Keytruda (pembrolizumab) • Lenvima (lenvatinib)
9d
Sunitinib for Advanced Thymus Cancer Following Earlier Treatment (clinicaltrials.gov)
P2, N=56, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2023 --> Jul 2024
Trial completion date • Metastases
|
Sutent (sunitinib)
9d
A Clinical Study of Surufatinib Combined With Chemotherapy as Neoadjuvant Treatment in Osteosarcoma (clinicaltrials.gov)
P2, N=160, Recruiting, Second Affiliated Hospital, School of Medicine, Zhejiang University | Not yet recruiting --> Recruiting | Initiation date: Jul 2023 --> Jan 2024
Enrollment open • Trial initiation date
|
cisplatin • Sulanda (surufatinib)
9d
HCCSC-C03: Disitamab Vedotin Combined With Fruquintinib for mCRC With HER2 Expression (clinicaltrials.gov)
P4, N=51, Active, not recruiting, Zhongnan Hospital | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Jan 2024 --> Jan 2025
Trial completion date • Trial primary completion date • Metastases
|
HER-2 (Human epidermal growth factor receptor 2)
|
HER-2 amplification • HER-2 mutation • HER-2 expression
|
Aidixi (disitamab vedotin) • Fruzaqla (fruquintinib)
9d
A Randomized, Double-Blind, Placebo-Controlled Trial Evaluating the Effect of Topical Urea for Secondary Prophylaxis of Hand Foot Skin Reaction in Renal Cell Cancer Patients on Sunitinib Therapy. (PubMed, Clin Genitourin Cancer)
The study suggested that the urea-based cream was not superior to placebo in decreasing the appearance of new HFSR in renal cancer patients receiving 4:2 regimen of sunitinib.
Clinical • Journal
|
KDR (Kinase insert domain receptor)
|
KDR rs1870377
|
Sutent (sunitinib)
9d
Clinical Study of the Safety and Efficacy of BAT5906 Injection (clinicaltrials.gov)
P1/2, N=60, Completed, Bio-Thera Solutions | Recruiting --> Completed | Trial completion date: Dec 2022 --> Nov 2023 | Trial primary completion date: Dec 2022 --> Nov 2023
Trial completion • Trial completion date • Trial primary completion date
|
VEGFA (Vascular endothelial growth factor A)
10d
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
|
everolimus • Lenvima (lenvatinib)
10d
Diagnosis and management of neuroendocrine tumours. (PubMed, Clin Med (Lond))
Treatment comprises surgery where curative resection is possible through to approaches where disease stabilisation is the key, involving somatostatin analogues, peptide receptor radionuclide therapy (PRRT), everolimus, sunitinib, liver-directed therapies and sometimes chemotherapy. Although local and systemic complications can occur, they are associated with reasonable 5- and 10-year survival rates, respectively.
Journal
|
SSTR (Somatostatin Receptor)
|
Sutent (sunitinib) • everolimus
13d
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
|
KIT (KIT proto-oncogene, receptor tyrosine kinase) • FLT1 (Fms-related tyrosine kinase 1)
|
KIT mutation
|
Lenvima (lenvatinib) • AiTan (rivoceranib) • Inlyta (axitinib)
13d
NCI-2015-01097: A Phase 2 Study of Cediranib in Combination With Olaparib in Advanced Solid Tumors (clinicaltrials.gov)
P2, N=122, Active, not recruiting, National Cancer Institute (NCI) | Terminated --> Active, not recruiting | Trial completion date: Jun 2022 --> Apr 2025
Enrollment closed • Trial completion date • Combination therapy • Metastases
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
|
HER-2 expression • ALK mutation
|
Lynparza (olaparib) • Recentin (cediranib)
14d
New P2/3 trial • Metastases
|
gemcitabine • AiRuiKa (camrelizumab) • albumin-bound paclitaxel • Sulanda (surufatinib)
14d
New P2 trial • Metastases
|
cisplatin • Lenvima (lenvatinib) • Loqtorzi (toripalimab-tpzi) • oxaliplatin
14d
New P2 trial
|
Lenvima (lenvatinib) • Kaitanni (cadonilimab)
14d
New P2 trial • Metastases
|
gemcitabine • albumin-bound paclitaxel • Sulanda (surufatinib)
16d
New P2 trial • Metastases
|
Tyvyt (sintilimab) • Stivarga (regorafenib) • Fruzaqla (fruquintinib)
16d
Sintilimab Injection Combined With Inlyta in Fumarate Hydratase- Deficient Renal Cell Carcinoma (clinicaltrials.gov)
P2, N=41, Active, not recruiting, West China Hospital | Recruiting --> Active, not recruiting | Trial primary completion date: Mar 2024 --> Mar 2025
Enrollment closed • Trial primary completion date
|
Tyvyt (sintilimab) • Inlyta (axitinib)
16d
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
|
KRAS (KRAS proto-oncogene GTPase)
|
KRAS mutation • KRAS G12C • KRAS G12
|
Lenvima (lenvatinib) • Lumakras (sotorasib)
17d
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
|
AFP (Alpha-fetoprotein) • FLT4 (Fms-related tyrosine kinase 4) • VEGFC (Vascular Endothelial Growth Factor C)
|
Lenvima (lenvatinib)
17d
Fulminant Clostridioides difficile infection during treatment with FLT3 inhibitor for acute myeloid leukemia (PubMed, Rinsho Ketsueki)
An 80-year-old man with FLT3-TKD mutation-positive acute myeloid leukemia (AML) relapsed during consolidation therapy with venetoclax/azacitidine and was started on gilteritinib as salvage therapy. The patient was discharged from the intensive care unit on the 18th day after the onset of CDI. We report this case not only due to the rarity of fulminant CDI during AML treatment, but also because it is a valuable example of effective treatment of fulminant CDI with fidaxomicin.
Journal
|
FLT3 (Fms-related tyrosine kinase 3)
|
FLT3-TKD mutation
|
Venclexta (venetoclax) • Xospata (gilteritinib) • azacitidine
17d
Trial completion date • Surgery
|
RET (Ret Proto-Oncogene)
|
Sutent (sunitinib)
18d
Treatment Access for Gastrointestinal Stromal Tumor in Predominantly Low- and Middle-Income Countries. (PubMed, JAMA Netw Open)
Gastrointestinal stromal tumor (GIST) is a rare cancer treated with the tyrosine kinase inhibitors imatinib mesylate or sunitinib malate. In this cohort study of patients with GIST who were predominantly from LMICs and received orally administered therapy through the GIPAP or MAS programs, outcomes were similar to those observed in high-resource countries. These findings underscore the feasibility and relevance of administering oral anticancer therapy to a molecularly defined population in LMICs, addressing a critical gap in cancer care.
Journal • Stroma
|
KIT (KIT proto-oncogene, receptor tyrosine kinase)
|
imatinib • Sutent (sunitinib)
19d
Oleuropein attenuates the nephrotoxic effect of sunitinib in rats: Unraveling the potential role of SIRT6/Notch-1/NLRP-3/IL-1β axis. (PubMed, Arch Biochem Biophys)
All these changes were almost alleviated by OLE co-treatment. These findings suggest the implication of SIRT6/Notch-1/NLRP3/IL-1β axis in the pathogenesis of SUN-induced nephrotoxicity and highlight OLE as a prospective renoprotective agent during SUN chemotherapy to halt its renal toxicity likely through promotion of SIRT6 and suppression of Notch-1/NLRP3/IL-1β signaling pathway.
Preclinical • Journal
|
NOTCH1 (Notch 1) • CCL2 (Chemokine (C-C motif) ligand 2) • IL1B (Interleukin 1, beta) • NLRP3 (NLR Family Pyrin Domain Containing 3) • SIRT6 (Sirtuin 6)
|
Sutent (sunitinib)
19d
Sweet syndrome induced by FLT3 inhibitors: case report and literature review. (PubMed, Hematology)
The FLT3 inhibitor gilteritinib was administered for reinduction therapy after failure of chemotherapy with a combination of venetoclax, decitabine, aclarubicin, cytarabine and granulocyte colony-stimulating factor. Similar cases of Sweet syndrome following FLT3 inhibitor therapy for acute myeloid leukemia were reviewed. Attention should be given to this rare complication when FLT3 inhibitors are used for acute myeloid leukemia therapy, and appropriate treatments need to be administered in a timely manner.
Review • Journal
|
FLT3 (Fms-related tyrosine kinase 3) • DNMT3A (DNA methyltransferase 1)
|
FLT3-ITD mutation • FLT3 mutation • DNMT3A mutation • DNMT3A mutation + FLT3-ITD mutation • FLT3‐ITD + DNMT3A mutation
|
Venclexta (venetoclax) • cytarabine • Xospata (gilteritinib) • decitabine • aclarubicin
21d
Trial completion date • Combination therapy
|
cisplatin • pemetrexed • Recentin (cediranib)
21d
Trial completion date • Stroma
|
KIT (KIT proto-oncogene, receptor tyrosine kinase)
|
KIT expression
|
sorafenib • imatinib • Sutent (sunitinib)
21d
Feature Engineering-Assisted Drug Repurposing on Disease-Drug Transcriptome Profiles in Gastric Cancer. (PubMed, Assay Drug Dev Technol)
Then, using the drug repurposing method with the Connectivity Map CLUE Query tools, potential drugs such as Forskolin, Gestrinone, Cediranib, Apicidine, and Everolimus, which showed a highly negative correlation with the expression levels of the selected genes, were identified. This study provides a method to develop new approaches to diagnosing and treating gastric cancer by comparing the transcriptome profiles of patients gastric cancer and performing a feature engineering-assisted drug repurposing analysis based on cancer data.
Journal
|
ETV3 (ETS Variant Transcription Factor 3)
|
everolimus • Recentin (cediranib)
21d
HMGB2 Release Promotes Pulmonary Hypertension and Predicts Severity and Mortality of Patients With Pulmonary Arterial Hypertension. (PubMed, Arterioscler Thromb Vasc Biol)
Smooth muscle cell (SMC)-specific HMGB2 knockout or HMGB2-OE (HMGB2 overexpression) mice and HMGB2 silenced rats were used to establish hypoxia+Su5416 (HySu)-induced PH mouse and monocrotaline-induced PH rat models, respectively...Our findings indicate that targeting HMGB2 might be a novel therapeutic strategy for treating PH. Serum HMGB2 levels could serve as a novel biomarker for diagnosing PA hypertension and determining its prognosis.
Journal
|
HMGB2 (High Mobility Group Box 2)
|
semaxanib (SU5416)