Safety and Pharmacokinetics of Oleylphosphocholine (OlPC), Administered Orally in Healthy Adults: A Phase 1, Single Center, Open-label, Staggered, Dose-escalation Trial

The goal of this interventional study is to assess the safety and tolerability of OlPC and to characterize the pharmacokinetics (PK) of OlPC following single, ascending doses administered orally in healthy-fed subjects.

Start Date21 Jun 2023

Sponsor / Collaborator

University Hospital Tübingen

100 Clinical Results associated with Oleylphosphocholine

100 Translational Medicine associated with Oleylphosphocholine

100 Patents (Medical) associated with Oleylphosphocholine

Literatures (Medical) associated with Oleylphosphocholine

05 Jul 2023·The Journal of antimicrobial chemotherapy

Efficacy of oleylphosphocholine in experimental cutaneous leishmaniasis.

Article

Author: Croft, Simon L ; Mcarthur, Kerri-Nicola ; Yardley, Vanessa ; Van Den Heuvel, Dennie ; Platteeuw, Johannes J ; Dixon, Jodie ; Harris, Andy ; Van Bocxlaer, Katrien ; Alavijeh, Mo

OBJECTIVESCutaneous leishmaniasis (CL) is a neglected tropical disease causing a range of skin lesions for which safe and efficacious drugs are lacking. Oleylphosphocholine (OLPC) is structurally similar to miltefosine and has previously demonstrated potent activity against visceral leishmaniasis. We here present the in vitro and in vivo efficacy of OLPC against CL-causing Leishmania species.METHODSThe antileishmanial activities of OLPC were evaluated and compared with miltefosine in vitro against intracellular amastigotes of seven CL-causing species. Following the confirmation of significant in vitro activity, the performance of the maximum tolerated dose of OLPC was evaluated in an experimental murine model of CL followed by a dose-response titration and the efficacy evaluation of four OLPC formulations (two with a fast-release and two with a slow-release profile) using bioluminescent Leishmania major parasites.RESULTSOLPC demonstrated potent in vitro activity of the same order as miltefosine in the intracellular macrophage model against a range of CL-causing species. A dose of 35 mg of OLPC/kg/day administered orally for 10 days was well-tolerated and able to reduce the parasite load in the skin of L. major-infected mice to a similar extent as the positive control paromomycin (50 mg/kg/day, intraperitoneally) in both in vivo studies. Reducing the dose of OLPC resulted in inactivity and modifying the release profile using mesoporous silica nanoparticles led to a decrease in activity when solvent-based loading was used in contrast to extrusion-based loading, which had no impact on its antileishmanial efficacy.CONCLUSIONSTogether, these data suggest that OLPC could be a promising alternative to miltefosine treatment for CL. Further investigations exploring experimental models with additional Leishmania species and skin pharmacokinetic and dynamic analyses are required.

06 Nov 2020·ChemSusChemQ2 · CHEMISTRY

Organic Ionic Plastic Crystal‐Based Composite Membranes for Light Gas Separation: The Impact of Varying Ion Type and Casting Method

Q2 · CHEMISTRY

Article

Author: Ramos, Fernando ; Forsyth, Maria ; Pringle, Jennifer M.

AbstractThe promise of organic ionic plastic crystals (OIPCs) for development of a novel type of gas separation membrane with competitive gas selectivity for CO2/N2 was recently demonstrated. This work aimed to design more selective membranes by investigating a different type of OIPC and a new membrane preparation method. Two different OIPCs were solvent‐cast or co‐cast with poly(vinylidene difluoride) (PVDF), and their gas transport properties were compared. The first OIPC, methyl(diethyl)isobutylphosphonium hexafluorophosphate ([P122i4][PF6]), was previously studied using the co‐cast method, and this was used as a benchmark. The second, N‐methyl‐N‐ethylpyrrolidinium bis(fluorosulfonyl)imide ([C2mpyr][FSI]), was investigated for the first time for gas separation applications, achieving high selectivities (α >40). The thermophysical properties of the composites indicated that the co‐casting method is a good way to fabricate solid, mechanically stable and durable membranes. Additionally, the enhanced molecular interactions indicated in OIPC/PVDF co‐cast composites point to a new approach for synthesis of other highly selective OIPC‐based membranes.

29 Jul 2019·Leukemia & Lymphoma

Oral azacitidine (CC-486) in combination with lenalidomide and dexamethasone in advanced, lenalidomide-refractory multiple myeloma (ROAR study)

Article

Author: Guzman, Roberto ; Kalff, Anna ; Bergin, Krystal ; Reynolds, John ; Thakurta, Anjan ; Spencer, Andrew ; Ren, Yan ; Khong, Tiffany ; Wang, Maria ; Mithraprabhu, Sridurga ; Bowen, Kathryn M. ; Couto, Suzana

In preclinical studies, oral azacitidine (CC-486), a hypomethylating agent, has been shown to have a direct anti-MM effect and in vitro anti-MM synergism when combined with lenalidomide (LEN). We present a phase 1b, single center, 3 × 3 dose escalation study with planned expansion at maximum tolerated dose (MTD), which assessed the safety and efficacy of combining CC-486 with LEN (25 mg d1-21/28) and dexamethasone (DEX) (40 mg weekly) in patients with relapsed/refractory MM who had previously failed LEN. Twenty-four patients were enrolled. The MTD of CC-486 was 150 mg d1-21; recommended expansion dose was 100 mg d1-21. Adverse events were predictable and manageable. ORR was 37.5%; clinical benefit rate was 50%. Median OS was 10.3 m; median PFS was 2.6 m. Correlative proteomics demonstrated that higher MM tumor cell cereblon expression (pretreatment, C1D5) was associated with superior PFS/OS. CC-486, LEN and DEX produced meaningful clinical responses in heavily treated LEN refractory MM patients. Proteomics may have utility in predicting clinical outcomes.

100 Deals associated with Oleylphosphocholine

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Indication	Highest Phase	Country/Location	Organization	Date
Chagas Disease	Phase 1	-	Max-Planck-Innovation GmbH	-
Chagas Disease	Phase 1	-	Dafra Pharma NV	-
Chagas Disease	Phase 1	Belgium	-	-
Leishmaniasis	Phase 1	-	Max-Planck-Innovation GmbH	-
Leishmaniasis	Phase 1	-	Dafra Pharma NV	-
Leishmaniasis	Phase 1	-	Dafra Pharma NV	-
Leishmaniasis	Phase 1	-	Max-Planck-Innovation GmbH	-
Mycoses	Phase 1	-	Max-Planck-Innovation GmbH	-
Mycoses	Phase 1	Belgium	-	-
Mycoses	Phase 1	-	Dafra Pharma NV	-

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