Sa·git·ta [ suh-jit-uh ]
noun, genitive
1. from Latin, literally: an arrow – such as the SagittaTM platform precisely points a target
2. the keystone of an arch – so as the SagittaTM platform is the backbone of RS Research
SagittaTM platform is a groundbreaking technology approach utilizing Polymer Drug Conjugates to target the tumor with a high payload of cytotoxics; resulting in high efficacy with reduced side-effect profile. In addition to moving our own candidates through clinical development, SagittaTM platform is available for co-development projects.
Clinicians have two types of pharmaceutical weapons while tackling cancer:
We combine both
↓
TARGETED “SMART” CHEMOTHERAPY
CHEMOTHERAPY
is effective
but due to toxicity,
dose is limited
TUMOR TARGETING
is well established
but not effective because,
not toxic enough
We combine both
↓
TARGETED “SMART” CHEMOTHERAPY
CLASSICAL CHEMOTHERAPY
TARGETED “SMART” CHEMOTHERAPY
RS Research currently develops two programs on the SagittaTM platform for targeted drug delivery: Bir & Dui.
The platforms carry multiple copies of the drug and a targeting moiety for directing the assembly to tumor tissue. Both platforms consist of highly flexible carriers: Size, linker, drug(s) and targeting moiety can all be rationally optimized. Biodegradable linker is tailored according to the drug of choice and the targeting moiety is selected matching the indication. The covalent conjugate is quite inactive in in vitro compared to the free drug, demonstrating its activity only after its cargo is released inside the targeted tumor cell. Active targeting of the toxic payload enables reduced side effect profile leading to higher compliance of patients, thus our motto:
SagittaTM Bir is a water-soluble platform where the amount of drug loading is determined by the hydrophobicity/hydrophilicity of the drug itself.
SagittaTM Dui consists of a block copolymer where the hydrophobicity of the drug enables formation of micellar constructs in aqueous environment. A second synergistic drug can be loaded non-covalently.
Both SagittaTM Bir and SagittaTM Dui Platforms use active Targeting which can be achieved via attachment of a variety of small molecules, antibodies or pieces thereof. Active targeting moieties recognize cell surface receptors. Drug carrier is internalized via endocytosis. Drug is released via cleavage of an enzyme sensitive linker or freely in the case of drug encapsulation
Why SagittaTM Platforms?
- Tunability: Soluble platform or micellar particle with size between 20-120 nm
- Prolonged circulation time: The elimination time and the systemic circulation prolongs because of polyethylene glycol (PEG) and the large molecular weight of the platform. Prolonged circulation time leads to higher accumulation at the diseased tissue.
- Diverse choice of drugs: Thanks to the flexible binding technology, in contrary to the similar competitors in the market, SagittaTM platform can be utilized with different chemotherapeutic agents. Cytotoxic payload can be changed for different target indications as well as potential synergistic therapeutic effect.
- Customized drug release: The linkers that connect the drug to the SagittaTM platform determine the rate of release of the native drug molecule. Importantly, drug release can be tuned and it can be driven by biological stimuli. Using SagittaTM, two different active pharmaceuticals with completely dissimilar release profiles can be generated to produce a synergistic therapeutic effect.
- Dual Drug Loading: SagittaTM can be utilized with different therapeutic modalities including small molecules, peptides, oligonucleotides, or possible combinations. This approach has the potential to enable the generation of synergistic therapies such as an anti-angiogenic + cytotoxic agent combination. With this approach, problems due to short half-life or high toxicity can be surmounted.
- High Drug Loading: Historically, drug conjugates have been limited to a drug loading capacity of less than 10%. SagittaTM platform can be loaded by over 50% by weight allowing for higher efficacy with maintained pharmacokinetic properties.
- Cellular targeting: In order to achieve the highest specificity, selective binding and maximum cellular internalization, SagittaTM nanoparticles can be combined with targeting moieties such as antibodies, antibody fragments, peptides, or other small molecular weight compounds. Targeting moiety selection is driven by the target tissue-type and cell characteristics.
- Manufacturing: A straight manufacturing process generates excellent yield and high purity material. The product can be sterilized by aseptic filtration. The product can be successfully scaled up to clinical GMP batches whilst retaining all its analytical and pharmaceutical properties.
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