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DRUG CLASS:

Farnesyl transferase inhibitor

1m
KURRENT-HN: Combination Trial of Tipifarnib and Alpelisib in Adult Recurrent/ Metastatic Head and Neck Squamous Cell Carcinoma (R/M HNSCC) (clinicaltrials.gov)
P1/2, N=45, Completed, Kura Oncology, Inc. | Active, not recruiting --> Completed | Trial completion date: Dec 2025 --> Jul 2025 | Trial primary completion date: Dec 2025 --> Jul 2025
Trial completion • Trial completion date • Trial primary completion date
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • HRAS (Harvey rat sarcoma viral oncogene homolog)
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Piqray (alpelisib) • Zarnestra (tipifarnib)
1m
Dapansutrile in multidisciplinary therapeutic applications: mechanisms and clinical perspectives. (PubMed, Front Pharmacol)
Furthermore, dapansutrile exhibits synergistic effects when combined with agents such as lonafarnib or immune checkpoint inhibitors, enhancing anti-inflammatory and anti-tumor responses. This review consolidates evidence on dapansutrile's molecular mechanisms, therapeutic applications, and biosafety, highlighting its potential as a novel, well-tolerated, and versatile anti-inflammatory agent. Future research should focus on optimizing its delivery, particularly to the central nervous system, and leveraging artificial intelligence to predict effective drug combinations.
Review • Journal
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IL18 (Interleukin 18) • IL1B (Interleukin 1, beta) • NLRP3 (NLR Family Pyrin Domain Containing 3)
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dapansutrile (OLT1177)
2ms
Using single-cell and transcriptome data to identify prognostic genes associated with SUMO-ylation and their molecular regulatory mechanisms in breast cancer. (PubMed, BMC Cancer)
In this study, 8 SUMO-ylation related prognostic genes were identified in BRCA, namely GPC1, CAPZA1, NUDCD1, MTDH, COX7A1, PLK3, FAM43A and CEBPD, offering fresh perspectives on the prognosis of BRCA.
Journal • BRCA Biomarker
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CD8 (cluster of differentiation 8) • BRCA (Breast cancer early onset) • GPC1 (Glypican 1) • FAM43A (Family With Sequence Similarity 43 Member A) • MTDH (Metadherin)
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sorafenib • Zarnestra (tipifarnib)
2ms
Integrative computational approach to farnesyltransferase inhibition toward anti-liver cancer drug candidate from Syzygium cumini essential oils. (PubMed, Mol Biol Res Commun)
However, MD simulations confirmed that both essential oil compounds exhibit binding stability comparable to that of Tipifarnib. Finally, α-humulene epoxide II and bornyl acetate from S. cumini exhibit favorable drug-like properties, high predicted safety margins, and a lack of organ-specific toxicity, underscoring their suitability for further drug development.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • MMP9 (Matrix metallopeptidase 9)
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Zarnestra (tipifarnib)
2ms
Farnesyltransferase inhibitors decrease matrix-vesicle-mediated mineralization in SaOS-2 cells. (PubMed, Mol Biol Rep)
Our findings demonstrate that FTIs Lonafarnib and Tipifarnib impair MVM, highlighting the essential role of farnesylation in biomineralization.
Journal
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COL1A1 (Collagen Type I Alpha 1 Chain) • RUNX2 (RUNX Family Transcription Factor 2)
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Zarnestra (tipifarnib)
3ms
Journal
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CCND1 (Cyclin D1) • YBX1 (Y-Box Binding Protein 1) • LYVE1 (Lymphatic vessel endothelial hyaluronan receptor 1) • SOX4 (SRY-Box Transcription Factor 4) • TCF4 (Transcription Factor 4)
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Zarnestra (tipifarnib)
4ms
The Fall of the Armor: Lamin Dysregulation and a Wide Network of Laminopathies. (PubMed, Subcell Biochem)
Lamins have also been shown to be dysregulated in a multitude of cancers, and research has uncovered a diabolical role of lamins in oncogenesis. The understanding of laminopathies and dysregulation of lamins resulting in disorders is critical in developing novel therapeutic strategies through drug repurposing and epigenetic modulation to curb the burden of the diseases.
Review • Journal
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LMNA (Lamin A/C) • LMNB2 (Lamin B2)
4ms
Wild-type RAS signaling is an essential therapeutic target in RAS-mutated cancers. (PubMed, Sci Signal)
The farnesyltransferase inhibitor tipifarnib blocked mutant HRAS-PI3K signaling and synergized with MEK inhibitors in HRAS-mutated cells, whereas KRASG12C inhibitors blocked mutant KRAS-MEK signaling and synergized with PI3K inhibitors in KRASG12C-mutated cells. Synergy was abolished in MEFs lacking all RAS proteins and in cancer cell lines in which nonmutated RAS family members were deleted. Our data highlight the critical role of wild-type RAS family members in supporting mutant RAS signaling and its importance as a therapeutic cotarget in RAS-mutated cancers.
Journal
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KRAS (KRAS proto-oncogene GTPase) • NRAS (Neuroblastoma RAS viral oncogene homolog)
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KRAS mutation • KRAS wild-type • RAS mutation • RAS wild-type • HRAS mutation • NRAS wild-type • NRAS G12
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Zarnestra (tipifarnib)
5ms
KURRENT-HN: Combination Trial of Tipifarnib and Alpelisib in Adult Recurrent/ Metastatic Head and Neck Squamous Cell Carcinoma (R/M HNSCC) (clinicaltrials.gov)
P1/2, N=40, Active, not recruiting, Kura Oncology, Inc. | Trial completion date: Jul 2025 --> Dec 2025 | Trial primary completion date: Jul 2025 --> Dec 2025
Trial completion date • Trial primary completion date
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • HRAS (Harvey rat sarcoma viral oncogene homolog)
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Piqray (alpelisib) • Zarnestra (tipifarnib)
7ms
Hepatitis D Virus Infection: Pathophysiology, Epidemiology and Treatment. Report From the Third Delta Cure Meeting 2024. (PubMed, Liver Int)
The improved knowledge of the HDV life cycle has led to the development and approval of the first HDV-direct antiviral, Bulevirtide (BLV)...Despite recent advances in antiviral treatment, strategies to achieve HBsAg loss, which most closely resembles HDV cure, are not available and antiviral treatment for patients with advanced liver disease is limited. The third international Delta Cure meeting, held in Milan in October 2024, aimed to share the latest findings, and this review highlights key takeaways from the lectures and research on HDV.
Review • Journal
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KEAP1 (Kelch Like ECH Associated Protein 1) • IFNA1 (Interferon Alpha 1)
9ms
HRAS Mutations in Head and Neck Carcinomas in Japanese Patients: Clinical Significance, Prognosis, and Therapeutic Potential. (PubMed, Int J Mol Sci)
HRAS knockdown with siRNA suppressed the in vitro migration ability of HRAS mutation-positive cells but not that of HRAS mutation-negative cells. In conclusion, a positive HRAS mutation could be an indicator of distant metastasis and poor prognosis, as well as a potential therapeutic target.
Journal
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HRAS (Harvey rat sarcoma viral oncogene homolog) • RAS (Rat Sarcoma Virus)
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RAS mutation • HRAS mutation
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Zarnestra (tipifarnib)
10ms
Enrollment closed
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • HRAS (Harvey rat sarcoma viral oncogene homolog)
|
Piqray (alpelisib) • Zarnestra (tipifarnib)