AMCIPATRICIN diascorbate (code SPK-843) is a new semi-synthetic, water-soluble polyene antibiotic, with potent broad-spectrum antifungal activity, particularly against Candida spp., Cryptococcus sp., and Aspergillus spp.

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Epidemiology of systemic fungal infections:

Fungal diseases are a public health issue: opportunistic infections (e.g. cryptococcosis and aspergillosis), hospital-associated infections (e.g. candidemia), and community-acquired infections pose an important threat to public health1. Globally, over 300 million people are afflicted with a serious fungal infection and 25 million are at high risk of dying or losing their sight2.

Mode of action:

Like other polyenes, the antifungal activity of AMCIPATRICIN is based on the destabilization of the cell membrane of sensitive organisms. The main mechanism of action is the reaction with sterols of the cell membrane which causes a leakage for low molecular, cytoplasmatic ingredients. The intracellular balance is then disturbed, ending up finally in cell extinction.


Extensive non-clinical data are available on AMCIPATRICIN and its salt with ascorbic acid.

  • Single dose toxicity (Rats),i.v.
  • Single dose toxicity (Cynomolgus Monkeys), i.v.
  • Single dose nephrotoxicity (Rabbits), i.v.
  • Repeated dose (2 weeks) toxicity study (Rats),i.v.
  • Repeated dose (4+4 weeks recovery) toxicity (Rats),i.v.a
  • Repeated dose (2 weeks) toxicity (Cynomolgus Monkeys) i.v.b
  • Repeated dose (4 weeks) toxicity (Cynomolgus Monkeys) i.v.c
  • Repeated dose (2 weeks) nephrotoxicity study in (Rabbits), i.v.
  • Repeated dose (13+4 weeks recovery time) toxicity (Rats), i.v., vs AmpB
  • Reproductive toxicology: Fertility and Early Embryonic Development (Rats), i.v.
  • Reproductive toxicology: Study of embryo-fetal development (Rats)
  • Genotoxicity: chromosomal aberrations (Chinese hamsters)
  • Genotoxicity: Peripheral blood micronucleus test (Mice), i.v.
  • Mutagenesis: bacterial reverse mutation assay (Ames test)
  • Vascular Irritation Study (Rabbits), 14 days, i.v.
  • Effects on action potential of right ventricular papillary muscle (Guinea pigs)
a. Vehicle: Glucose and Intralipid - b. Vehicle: Intralipid - c. Vehicle: Glucose
d. Lung fibroblast cells

NON-CLINICAL Safety Pharmacology Studies:

Safety Pharmacology Study in comparison with other polyene (general signs and behavior, CNS, autonomic nervous system and smooth muscles, peripheral nervous system, gastrointestinal system, cardiovascular system and the respiratory system, water and electrolyte metabolism, blood, pyrogenic effect in rabbits).

NON-CLINICAL Efficacy Pharmacology Studies

  • Candida albicans (Rats)
  • Pulmonary aspergillosis (Mice)
  • Cryptococcal meningoencephalitis (Mouse)
  • Pharmacokinetics after multiple doses (4 weeks) i.v. (Rats)



Proven in-vitro antifungal activity against:

  • Candida spp (albicans, glabrata, tropicalis, krusei, guilliermondii, kefyr, parapsilosis, stellatoidea, utilis, clinical isolates of Candida auris)
  • Non-Candida yeast tested (Cryptococcus neoformans, C. laurentii, Saccharomyces cerevisiae, Trichosporon beigelii, Rhodotorula pilimanae)
  • Filamentous fungi (Aspergillus spp., Paecilomyces variottii, Penicillium spp.,Sporothrix schenkii, Mucor sp., Rhizopus oryzae, Microsporum spp., Trichophyton spp.)

Human clinical studies:

Phase I Studies

  • A Single Ascending Dose Pilot Study in Healthy Adult Males (i.v.)
  • Human Pharmacology Study with Repeated Dose (14 days) by (i.v.) in Healthy Male Volunteers

Phase II Studies

  • Efficacy, safety, and PK in patients with deep mycosis (chronic necrotizing pulmonary aspergillosis and pulmonary cryptococcosis) (Exploratory study: multicenter, open-label, uncontrolled, i.v.)
  • An open-label, dose-escalation pilot study to investigate the safety and efficacy of SPK-843 (AMCIPATRICIN) i.v., in the treatment of esophageal candidiasis in HIV-infected patients.

Main overall outcomes:

  • Relative acute toxicity in mice, rats, and monkeys lower than other polyenes.
  • 13-week toxicity study: no evidence of serious nephrotoxicity even at the highest dose (5 mg/kg).
  • Non-toxic dose level: 0.2 mg/kg b.w. in rats (13-weeks i.v. toxicity study)


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BEYOND THE PRESENT: Bioseutica® is in the advanced R&D development of AMCIPATRICIN by inhalation for treatment and/or prophylaxis of severe fungal infections in cystic fibrosis and/or immunocompromised patients (Patent pending). WE ARE LOOKING FOR BUSINESS PARTNERS.