Biological profile

crRASP is a multipotent conjugate of the naturally occurring all-trans-retinoic acid and the polyamine spermine that addresses the major challenges of current treatments: not toxic or teratogenic not irritant to skin and eyes not phototoxic not mutagenic does not induce chromosome aberration

Synthesis

Two-step, high-yielding, fast & easy to perform at ambient temperature manfuacturing process: Readily upscaled Atom economic Analytical grade(crRASP purity >98%)

Intellectual property

crRASP is a patented and secured compound:

  • Crystalline Forms for salts of N1,N12-DI(all-trans-retinoyl)spermine, Processes for their production and pharmaceutical compositions thereof. EP3878840A1/15-09-2021 Patent pending.
  • Κρυσταλλικές μορφές της Ν1,Ν12-δι(all-trans-ρετινοϋλο)σπερμίνης, διεργασίες για την παραγωγής τους και φαρμακευτικές συνθέσεις αυτών. GR20200100131/10-03-2020 Patent granted.

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Scientific Evidence of RASP:

Safety in rats:
RASP administered orally at 50 mg/kg to rats over two generations did not show any adverse effects on growth, characteristics, reflexes, or organ health.
Anti-inflammatory effects:
RASP demonstrated four times more potent anti-inflammatory effects on rat paw edema compared to tretinoin in a comparative in vivo study. This suggests potential efficacy in managing inflammatory conditions.
Inhibition of lipoxygenase:
RASP exhibited potent inhibitory effects on lipoxygenase, a crucial component of a biochemical pathway involved in inflammation and immune response. This mechanism further supports its potential as an anti-inflammatory agent.
Immunosuppressant potential:
RASP significantly inhibits the production of IL-2 and IFN-γ by CD4+ and CD8+ cells, indicating potential as an immunosuppressant drug. This property could be beneficial in managing immune-mediated disorders.
Angiogenesis inhibition:
Both tretinoin and RASP dose-dependently inhibited angiogenesis, with RASP being more effective and having a wider dose range due to lower toxicity compared to tretinoin. This suggests a potential application in diseases characterized by abnormal angiogenesis, such as cancer.
Cytotoxicity on cancer cells:
RASP was less cytotoxic than tretinoin on HUVEC cells but more effective and potent on prostate cancer cells. This indicates a promising role for RASP in cancer therapy, potentially with a better safety profile than tretinoin.
Inhibition of RNase P:
RASP inhibits RNase P, a key enzyme in protein synthesis, at lower concentrations than retinoids. This suggests potential effectiveness in treating skin conditions requiring increased protein synthesis, such as psoriasis.
Effectiveness against cancer:
RASP has demonstrated effectiveness against cancer by regulating the expression of genes and miRNAs involved in apoptosis and the cell cycle. This suggests its potential as a therapeutic agent in cancer treatment.

Research Publications:

  1. Petridis T., Giannakopoulou D., Stamatopoulou V., Grafanaki K., Kostopoulos C.G., Papadaki H., Malavaki C.J., Karamanos N.K., Douroumi S., Papachristou D., Magoulas G.E., Papaioannou D., Drainas D. “Investigation on Toxicity and Teratogenicity in Rats of a Retinoid-Polyamine Conjugate with Potent Anti-Inflammatory Properties”. Birth Defects Research (Part B) 107 (2016) 32-44.
  2. Hadjipavlou-Litina D., Magoulas G.E., Bariamis S.E., Drainas D., Avgoustakis K., Papaioannou D. “Does conjugation of antioxidants improve their antioxidative/anti-inflammatory potential?” Bioorganic & Medicinal Chemistry 18 (2010) 8204-8217.
  3. Papaioannou D., Drainas D., Tsambaos D., WO 2004/018001 A1; US 7,517,913 B2
  4. Vourtsis D., Lamprou M., Sadikoglou E., Giannou A., Theodorakopoulou O., Sarrou E., Magoulas G.E., Bariamis S.E., Athanassopoulos C.M., Drainas D., Papaioannou D., Papadimitriou E. “Effect of an all-trans-retinoic acid conjugate with spermine on viability of human prostate cancer and endothelial cells in vitro and angiogenesis in vivo”. European Journal of Pharmacology 698 (2013) 122-130.
  5. Magoulas G., Papaioannou D., Papadimou E., Drainas D. “Preparation of spermine conjugates with acidic retinoids with potent ribonuclease P inhibitory activity: European Journal of Medicinal Chemistry 44 (2009) 2689-2695.
  6. Grafanaki K., Skeparnias I., Kontos C.K., Anastasakis D., Korfiati A., Kyriakopoulos G., Theofilatos K., Mavroudi S., Magoulas G., Papaioannou D., Scorilas A., Stathopoulos C., Drainas D. “Pharmacoepigenomics circuits induced by a novel retinoid-polyamine conjugate in human immortalized keratinocytes” Pharmacogenomics J. 21 (2021) 638-648.

Inventors: