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.

Start Date01 Jul 2009

Sponsor / Collaborator

Esperance Pharmaceuticals, Inc.

100 Clinical Results associated with Onvitrelin Ucalontide

100 Translational Medicine associated with Onvitrelin Ucalontide

100 Patents (Medical) associated with Onvitrelin Ucalontide

Literatures (Medical) associated with Onvitrelin Ucalontide

01 Jan 2022·Clinical oral investigationsQ2 · MEDICINE

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

Q2 · MEDICINE

Article

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

OBJECTIVES:

The 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 METHODS:

Fifteen 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.

RESULTS:

Articaine (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.

CONCLUSIONS:

Single 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 RELEVANCE:

Single 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.

01 Feb 2021·Gynecologic oncologyQ2 · MEDICINE

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

Q2 · MEDICINE

Article

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

OBJECTIVE:

This 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.

METHODS:

In 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).

RESULTS:

Forty-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.

CONCLUSIONS:

ORR 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.

01 Nov 2020·Molecular cancer therapeuticsQ2 · MEDICINE

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

Q2 · MEDICINE

Article

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

Abstract:

Here, 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.

News (Medical) associated with Onvitrelin Ucalontide

06 Oct 2015

·www.biospace.com

MD Anderson Cancer Center and Theraclone Launch New Immuno-Oncology Company OncoResponse with $10 Million Series A

October 7, 2015 By Mark Terry , BioSpace.com Breaking News Staff MD Anderson Cancer Center , located in Houston, Texas, announced yesterday that together with Seattle-based Theraclone Sciences, Inc. , it was launching an immuno-oncology antibody discovery company, OncoResponse . In addition, OncoResponse closed a Series A financing round worth $9.5 million, co-led by ARCH Venture Partners , Canaan Partners and MD Anderson . Also participating were William Marsh Rice University and Alexandria Real Estate Equities . The startup will utilize Theraclone ’s I-STAR immune screening platform to identify potential therapeutic antibodies against novel targets culled from immuno-oncology patients. This technology screens antibodies produced by the human body in order to identify those that have particular sensitivity and reactivity that might be useful for cancer drugs. MD Anderson will provide samples from willing patients, as well as clinical data in patients that respond well to therapies. If any of OncoResponse ’s products make it to clinical trials, they will be performed at MD Anderson . “The immune system of patients who have responded exceptionally well to cancer immunotherapies may hold the key within their memory repertoire as to what gives them an edge over other patients with less robust immune responses,” said Clifford Stocks , chief executive officer of Theraclone and interim chief executive officer of OncoResponse in a statement. “It could provide us with a way to increase success rates in treating cancer. I-STAR immune repertoire screening technology has the unique capability to identify rare cancer-fighting antibodies and new targets. We’re extremely excited to have teamed up with MD Anderson experts to make a difference in the lives of patients with cancer and their families.” In April, Theraclone announced that it was using its human memory B-cell interrogation platform, in other words I-STAR, to identify possible therapeutic antibodies against the Ebola virus. That project is part of a consortium formed by Seattle-based BIO Ventures for Global Health , along with a number of Ebola experts. Theraclone received up to $4.4 million in a Series C financing round, including an investment from the Wellcome Trust . MD Anderson has been active in biotech-related company development recently. On Aug. 26, The University of Texas MD Anderson Cancer Center inked a deal with Germany-based Immatics Biotechnologies GmbH to launch Immatics US Inc. This company will develop adoptive cellular therapies (ACT) to treat a variety of cancer. Immatics US launched with $60 million, of which $40 million came from Immatics Biotechnologies and $19.7 million came from grants from the Cancer Prevention and Research Institute of Texas . MD Anderson , also in August, formed an alliance with Esperance Pharmaceuticals, Inc. to push development of its lead anti-cancer candidate EP-100 for ovarian cancer. It also penned a deal with Merck & Co. to evaluate anti-PD-1 therapy Keytruda in combination with other drugs and cancer treatments. Immuno-oncology is the hot new area for cancer treatment. At its most basic, it programs the patient’s immune system to attack specific cancer cells. There has also been significant work on so-called checkpoint inhibitors. Cancer cells create molecules that prevent the body’s immune system from working effectively. By stimulating and programming immune cells while simultaneously blocking the tumor cell’s ability to put the brakes on the immune system, immuno-oncology is showing great promise and is the focus of a lot of research. Companies making headway in this area include AstraZeneca PLC , MedImmune , Sanofi and Regeneron Pharmaceuticals, Inc. . Regeneron Pharmaceuticals, Inc. and Roche , and Roche , to name just a few. “The field of immuno-oncology has shown the potential to dramatically improve outcomes for patients with certain types of cancer,” said George Yancopoulos , chief scientific officer of Regeneron and president of Regeneron Laboratories in a July 2015 statement regarding a collaboration with Sanofi . “However, the field is still in its very early days. We believe the approaches most likely to deliver the best results to patients will combine multiple innovative therapies acting on different pathways and targets both in the tumor and the body’s immune response—and will precisely target these medicines to the right patient.” MD Anderson and Theraclone ’s spinoff, OncoResponse , will have headquarters in Houston. It is reportedly hiring five to 10 employees.

Immunotherapy

26 Aug 2015

·www.biospace.com

Immatics US Launches as Spinout of Immatics and MD Anderson Cancer Center

August 26, 2015 By Alex Keown , BioSpace.com Breaking News Staff HOUSTON -- The University of Texas MD Anderson Cancer Center teamed up with Germany-based Immatics Biotechnologies GmbH to launch Immatics US Inc. , which is aimed at developing adoptive cellular therapies (ACT) for the treatment of a number of cancers. Immatics US will launch with a war chest of more than $60 million, which includes $40 million from Immatics Biotechnologies and $19.7 million in grant money from the Cancer Prevention and Research Institute of Texas . The new company will be led by Hapreet Singh , the co-founder of Immatics Biotechnologies . Using the technologies at its disposal, Singh said Immatics has “discovered dozens of novel immunotherapy targets” for the company to explore. “With several complementary development programs guided by some of the most exceptional scientists in the field of cancer immunotherapy, we are in exactly the right place to deliver transforming therapies to cancer patients with high medical need,” Singh said in a statement. In addition to Singh, company leaders include Steffen Walter , who will be the chief scientific officer, Toni Weinschenk , chief technology officer, and Carsten Reinhardt chief medical officer. There was no indication of how many other employees Immatics U.S. would employ or already has employed. MD Anderson has a history of forming alliances with large pharmaceutical companies. Earlier this month MD Anderson announced an alliance with Esperance Pharmaceuticals, Inc. to accelerate the clinical development of its lead anti-cancer candidate EP-100 for the treatment of ovarian cancer. Additionally, MD Anderson struck a deal with Merck & Co. to evaluate its blockbuster anti-PD-1 therapy Keytruda in combination with other treatments, such as chemotherapy, radiation therapy and other antitumor medicines. Immatics U.S. will capitalize on its parent company’s technology platform XPRESIDENT for the “discovery and further qualification” of “highly specific cancer targets that can be used as the basis for a range of cancer immunotherapy applications including ACT.” The new company will develop three different ACT approaches for the treatment of tumors with high un-met medical needs, the first of which will enter the clinic in 2016. The three approaches include ACTolog, ACTengine and ACTallo. The ACTolog process involves selecting, enriching and the ex-vivo expansion of a patient’s endogenous T cells specifically recognizing Immatics’ XPRESIDENT targets. ACTengine involves genetically engineering a patient’s own T cells to express novel T-cell receptors which are specific to Immatics’ XPRESIDENT targets, the company said. ACTallo is an allogenic approach that will use off-the-shelf T cells that have been engineered to express novel T-cell receptors. Immatics US, Inc. will develop both autologous and allogenic ACT approaches by capitalizing on MD Anderson ‘s clinical oncology and cell therapy programs and Immatics’ cancer target and T-cell receptor (TCR) discovery capabilities, the new company said in a statement this morning. The new company will use MD Anderson ’s cytokine IL-21 for expansion of T cells, which is a gamma-delta T-cell platform for allogeneic cell therapy approaches and various technologies designed to optimize the development of ACT. “This capability will enable Immatics US, Inc. to develop TCR-based approaches and to have complementary utility with other approaches for addressing tumor targets. Immatics believes its ACT will be both efficacious and safe due to the specificity of its novel well-characterized targets, including novel over-expressed, cancer-testis and neo-antigens ideally suited for specific and safe ACT approaches,” the company said in a statement.

ImmunotherapyCell Therapy

100 Deals associated with Onvitrelin Ucalontide

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Indication	Highest Phase	Country/Location	Organization	Date
Ovarian Cancer	Phase 2	United States	Esperance Pharmaceuticals, Inc.	06 Jun 2012
Advanced Malignant Solid Neoplasm	Phase 1	United States	Esperance Pharmaceuticals, Inc.	01 Jul 2009
Pancreatic Cancer	Preclinical	United States	Pennington Biomedical Research Center	15 Apr 2011

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2015	Phase 2	Recurrent ovarian cancer	44	EP-100 + paclitaxel	quaudfnjfn(jkgnovvlyx) = ehesglipef jimgxhconv (zyspsyxanb, 51.6 - 89.8) View more	-	20 May 2015
ASCO2015	Phase 2	Recurrent ovarian cancer	44	paclitaxel	quaudfnjfn(jkgnovvlyx) = cddlikbssk jimgxhconv (zyspsyxanb, 47.8 - 88.7) View more	-	20 May 2015
ASCO2012	Phase 1	-	37	EP-100	evkcgpjsjk(mwrogsoqzs) = stable disease for >12 weeks in 5 pts bqlaxyqgxy (cprzlxxeut )	-	20 May 2012
AACR2012	Phase 1	Non-Hodgkin Lymphoma	-	EP-100	wkyhqqiwnt(mdkivvmqnp) = rhljsnvxwn vffcflvlhq (nnagrkivcu ) View more	-	15 Apr 2012

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