A Phase 1, Multi-center, Open-label, Dose-escalation, Safety, Pharmacodynamic and Pharmacokinetic Study of EP-100 Given Intravenously 3 Out of 4 Weeks in Subjects With Advanced Solid Tumors

This study is being done to:
Test the safety of EP-100 and see what effect (good and bad) it has on the patient and their cancer;
Find the highest dose of EP-100 that can be given without causing bad side effects;
Examine how much EP-100 is in the blood at certain times after it is given and how quickly the body gets rid of it;
Observe whether there is any effect of EP-100 on the size and activity of cancer in the patient's body.

开始日期2009-07-01

申办/合作机构

Esperance Pharmaceuticals, Inc.

100 项与 Onvitrelin Ucalontide 相关的临床结果

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项与 Onvitrelin Ucalontide 相关的文献（医药）

2022-01-01·Clinical Oral Investigations2区 · 医学

The effect of single buccal infiltration anesthesia of 4% articaine with either 1:100,000 or 1:200,000 epinephrine on pulpal blood flow and anesthesia of maxillary first molars and second premolars in humans

2区 · 医学

Article

作者: Krongyoungyuen, Piyatida ; Kijsamanmith, Kanittha ; Sriworapongpun, Chayanit ; Huayhongthong, Nadpatchamon ; Samdrup, Tshering ; Sakulyuenyong, Thanawin ; Pawasut, Nichanan

OBJECTIVESThe aim of this study was to determine the effect of single buccal infiltration of 4% articaine with either 1:100,000 (EP100) or 1:200,000 (EP200) epinephrine on pulpal blood flow (PBF), pulpal anesthesia and soft tissue anesthesia of maxillary first molars and second premolars in human subjects.MATERIALS AND METHODSFifteen healthy volunteers with intact maxillary first molars and second premolars received an infiltration of 4% articaine with either EP100 or EP200 at buccal aspect of maxillary first molars. The PBF, pulpal anesthesia and soft tissue anesthesia were assessed with a laser Doppler flowmeter (LDF), an electric pulp tester (EPT) and Aesthesiometer II, respectively.RESULTSArticaine (4%) with either EP100 or EP200 produced PBF reduction in maxillary first molars (injected teeth) by 68.09 and 69.83%, and produced PBF reduction in second premolars (adjacent teeth) by 76.81 and 75.02%, respectively at 15 min post injection. Duration of PBF returned to baseline was 159.00 ± 21.06 (EP100) and 159.00 ± 31.97 (EP200) min in the molars, and 161.00 ± 20.02 (EP100) and 159.00 ± 25.86 (EP200) min in the premolars. The onset of pulpal anesthesia was 2.80 ± 1.26 (EP100) and 3.07 ± 1.28 (EP200) min in the molars, and 2.13 ± 0.52 (EP100) and 2.40 ± 0.83 (EP200) min in the premolars; the duration of pulpal anesthesia was 74.53 ± 24.16 (EP100) and 76.27 ± 34.03 (EP200) min in the molars, and 82.53 ± 31.03 (EP100) and 75.60 ± 37.17 (EP200) min in the premolars. Buccal tissue anesthesia was found in both teeth (100%), but palatal anesthesia was achieved by 13.33% in the premolars and 6.67% in the molars for each solution.CONCLUSIONSSingle buccal infiltration to maxillary first molar produced PBF reduction and successful pulpal anesthesia, evaluated by EPT, in both first molar and second premolar. This anesthetic technique also produced high success of buccal tissue anesthesia, but demonstrated very low success for palatal tissue anesthesia.CLINICAL RELEVANCESingle buccal infiltration to maxillary first molar is potent enough for pulpal and buccal tissue anesthesia, except palatal tissue anesthesia, in both first molar and second premolar.

2021-02-01·Gynecologic Oncology2区 · 医学

A multicenter open-label randomized phase II trial of paclitaxel plus EP-100, a novel LHRH receptor-targeted, membrane-disrupting peptide, versus paclitaxel alone for refractory or recurrent ovarian cancer

2区 · 医学

Article

作者: Gordinier, Mary ; Leuschner, Carola ; Chelariu-Raicu, Anca ; Bavisotto, Linda ; Nick, Alpa ; Molin, Graziela Zibetti Dal ; Coleman, Robert L ; Urban, Renata ; Whisnant, John K

OBJECTIVEThis randomized open-label phase II study evaluated the safety and clinical activity of EP-100 plus weekly paclitaxel in patients with recurrent ovarian cancer expressing positive LHRH receptor.METHODSIn a limited "run-in" dose escalation phase for EP-100, six patients were treated with ascending dose levels (13 mg/m², 20 mg/m², 30 mg/m²). In the randomized phase, patients received weekly paclitaxel (80 mg/m² intravenously) plus twice weekly EP-100 (30 mg/m² intravenously; combination arm) or weekly paclitaxel alone (80 mg/m² intravenously; paclitaxel arm). The primary study endpoint was overall response rate (ORR).RESULTSForty-four patients were then randomized to either the experimental combination arm (n = 23) or the standard of care paclitaxel monotherapy arm (n = 21). The ORR was 35% (95%CI 16%-57%) for the combination arm and 33% (95% CI 15%-57%) for the paclitaxel arm. An interesting observation from an unplanned analysis was that a subset of patients with target liver lesions showed a greater overall response rate to the combination (69%) compared to paclitaxel alone (16%). The frequency of treatment-related grade 3-4 adverse events was similar between treatment arms: 48% vs 43% for the combination and paclitaxel arms, respectively.CONCLUSIONSORR in the EP-100 combination arm was similar to that in the group treated with paclitaxel alone; however, a subset of patients with liver metastases appeared to benefit from the combination. The addition of EP-100 did not appear to augment the adverse event profile of paclitaxel and was well tolerated.

2020-11-01·Molecular Cancer Therapeutics2区 · 医学

Enhanced Immunotherapy with LHRH-R Targeted Lytic Peptide in Ovarian Cancer

2区 · 医学

Article

作者: Coleman, Robert L. ; Chelariu-Raicu, Anca ; Ma, Shaolin ; Alila, Hector W. ; Sood, Anil K. ; Kim, Mark Seungwook ; Leuschner, Carola ; Lee, Sanghoon

AbstractHere, we examined the role of EP-100 [luteinizing hormone-releasing hormone (LHRH) ligand joined to a lytic peptide], improving the efficacy of immune checkpoint blockade. LHRH-R–positive murine ovarian cancer cells (ID8, IG10, IF5, and 2C12) were sensitive to EP-100 and were specifically killed at low micromolar levels through LHRH-R. EP-100 increased PD-L1 levels on murine ovarian cancer cells. In vivo syngeneic mouse models (ID8 and IG10) demonstrated that single-agent EP-100 reduced tumor volume, tumor weight, and ascites volume. The greatest reductions in tumor and ascites volume were observed with the combination of EP-100 with an anti–PD-L1 antibody. Immune profiling analysis showed that the population of CD8+ T cells, natural killer cells, dendritic cells, and macrophages were significantly increased in tumor and ascitic fluid samples treated with anti–PD-L1, EP-100, and the combination. However, monocytic myeloid suppressor cells, B cells, and regulatory T cells were decreased in tumors treated with anti–PD-L1, EP-100, or the combination. In vitro cytokine arrays revealed that EP-100 induced IL1α, IL33, CCL20, VEGF, and Low-density lipoprotein receptor (LDLR) secretion. Of these, we validated increasing IL33 levels following EP-100 treatment in vitro and in vivo; we determined the specific biological role of CD8+ T-cell activation with IL33 gene silencing using siRNA and Cas9-CRISPR approaches. In addition, we found that CD8+ T cells expressed very low level of LHRH-R and were not affected by EP-100. Taken together, EP-100 treatment had a substantial antitumor efficacy, particularly in combination with an anti–PD-L1 antibody. These results warrant further clinical development of this combination.

100 项与 Onvitrelin Ucalontide 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
卵巢癌	临床2期	美国	Esperance Pharmaceuticals, Inc.	2012-06-06
晚期恶性实体瘤	临床2期	美国	Esperance Pharmaceuticals, Inc.	2009-07-01

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临床结果

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ASCO2015	临床2期	复发性卵巢癌	44	EP-100 + paclitaxel	(齋襯齋糧鏇積膚鏇夢築) = 糧繭艱遞遞齋鬱襯醖遞夢衊製糧鏇齋築餘構範 (襯鹹夢廠窪選鹽夢築糧, 51.6 ~ 89.8) 更多	-	2015-05-20
ASCO2015	临床2期	复发性卵巢癌	44	paclitaxel	(齋襯齋糧鏇積膚鏇夢築) = 鑰鬱築範積鑰憲壓鬱鏇夢衊製糧鏇齋築餘構範 (襯鹹夢廠窪選鹽夢築糧, 47.8 ~ 88.7) 更多	-	2015-05-20
ASCO2012	临床1期	肿瘤	37	EP-100	(壓範製憲構餘願鬱醖齋) = stable disease for >12 weeks in 5 pts 構觸壓構願餘齋齋壓遞 (鬱範鏇簾憲鬱遞觸衊繭 )	-	2012-05-20
AACR2012	临床1期	非霍奇金淋巴瘤	-	EP-100	築構遞鑰衊網簾淵積窪(衊醖積繭憲蓋鹽夢膚膚) = 觸鹽鑰艱襯鹽網艱網積鹹遞選獵糧鹽鏇選夢鏇 (顧鏇艱築簾顧繭衊鏇糧 ) 更多	-	2012-04-15