Antibody, linker-payload, conjugation and analytics – we provide a one-stop solution for ADC discovery and development.
We understand the dynamic nature of the current ADC technology landscape and the complexities associated with it. Our team is well versed with a wide range of ADC technologies and is capable of adapting new technologies to support our client needs. We also provide expertise to develop novel liker technologies and cytotoxic payload optimization.
We offer a wide range of ADC services, and our team is competent at adapting new technologies to meet client requirements.
Linker Technologies
We offer services for designing and synthesizing ADC linkers and linker-drug conjugates. Based on the drug release mechanism, we design & synthesize different ADC linkers: Cleavable and non-cleavable linkers, self-immolation tracer-free linkers, and peptide linkers.
Conjugation Technologies
Our team carries out ADC conjugation services to accelerate the production of ADC constructs with quality attributes.
Amine (Lys) conjugation, thiol (Cys) conjugation, site-specific conjugation, enzymatic conjugation, glycoconjugation and click chemistry.
Payloads
According to clients’ requirements, we optimize payloads such as cytotoxic, non-cytotoxic, and biological payloads. Our team handles a wide range of cytotoxic payloads, including:
- Auristatins (MMAE and MMAF)
- Tubulysin
- PBD Dimer
- Maytansinoids (DM-1, DMO4)
- Duocarmycin
- Exatecans
ADC Discovery (Therapeutics and Tools or Reagents) and Development
Our ADC discovery programs are customized as per the target biology and desired mechanism of action. Specific screening strategies are designed and employed at a stage as early as antibody generation. Some of the early stage activities include screening and design of mAbs for internalization (or lack of it), effector function, off-site localization and half-life.
Rapid and comprehensive scouting of the linker-payload technology space can be plugged-in to identify the most desirable combinations of mAb, linker-payload and conjugation strategies. Stage appropriate in vitro screening and detailed evaluation of lead ADC molecules is carried out using customized assay platforms.
We also provide in vivo therapeutic evaluation, PK, and rodent toxicology assessment support for ADC candidates with appropriate bioanalytical methods customized for each program. Conjugation and purification process development takes into account each component of the ADC molecule. Quality, scalability, safety and cost-effectiveness concerns are addressed at each stage of process development.
ADC Analysis
A biomolecule is complex as an ADC and demands analytical assessment to ensure safety and quality. Routinely determined attributes during ADC analysis are
- DAR average
- Free-drug
- Conjugation site
- Aggregation
- Fragmentation
- Endotoxin
- Antigen binding affinity
- Plasma stability
- In vitro potency
Why Aurigene Pharmaceutical Services?
Site-specific conjugation technology
In-house linker library and Payload
Collaborative and solution driven
Analytical assessment to ensure safety and quality
Various commercial and customized linkers
Virtual Tour
Hyderabad R and D Center
Bangalore R and D Center
Resources
JULY 02, 2021
Oligonucleotide as a novel class of therapeutic modality
Oligonucleotides as a therapeutic class is a revolutionary approach to discover new and important therapeutic agents for treating human diseases. RNA-based intervention at times works in cases where other modalities do not work. For example, it may help in treating inborn errors in metabolism, genetic disorders and rareOligonucleotide therapeutics is the use of c...
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HPAPI Molecule from Development to Market
The global Highly Potent Active Pharmaceutical Ingredients (HPAPI) market is expected to reach USD 26.84 Billion by 2023 from USD 17.72 Billion in 2018, at a CAGR 8.7%....
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Systematic formulation design - shorten development cost & time
Project Challenge: Existing formulation (lower strength - 50 mg) was manufactured using direct compression process. This formulation posed poor powder flow and content uniformity issues during scale-up. Development of new strength 150 mg without any process issues was a challenge. Solution design: Preliminary pre-formulation, stress study and PSD impact assessmen...
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An efficient and convenient protocol for the synthesis of tetracyclic isoindolo[1,2-a]quinazoline derivatives
2016
A convenient and one-pot synthesis of tetracyclic isoindolo [1,2-a]quinazoline derivatives via Lewis acid mediated sequential C–N bond formation reactions is reported. This protocol provides a simple and rapid strategy for the synthesis of 12-benzylidene-10,12-dihydroisoindolo[1,2-b]quinazoline derivatives. However, a variety of tetracyclo indole fused quinazol...
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Alternate end-game strategies towards Nirmatrelvir synthesis: Defining a continuous flow process for the preparation of an anti-COVID drug
2005
Scalable alternate end-game strategies for the synthesis of the anti-COVID drug molecule Nirmatrelvir (1,PF-07321332) have been described. The first involves a direct synthesis of 1 via amidation of the carboxylic acid 7 (suitably activated as a mixed anhydride with either pivaloyl chloride or T3P) with the ...
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Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
2005
Mutations in MEK1/2 have been described as a resistance mechanism to BRAF/MEK inhibitor treatment. We report the discovery of a novel ATP-competitive MEK1/2 inhibitor with efficacy in wildtype (WT) and mutant MEK12 models. Starting from a HTS hit, we obtained selective, cellularly active ...
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Synthesis of Anti-covid Drug Nirmatrelvir Using Flow Chemistry
2005
Synthesis of the anti-covid therapeutic Nirmatrelvir by using flow chemistry to enhance efficiency of amide to nitrile conversion in a functionally and Stereochemically Embellished environment. ...
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