Following the latest scientific progress and regulatory guidelines, Creative Biolabs brings out an integrated series of in vitro drug-drug interaction testing services during early optimization phase for our worldwide customers.

As there is increasing population taking multiple medications, adverse drug-drug interactions (DDI) has become a crucial issue. If a certain component of drug A changes the activity of enzymes or transporters involved in the metabolism of drug B, it may either reduce the therapeutic efficacy or enhance the toxicity of drug B, leading to severe clinical consequences. Hence, to avoid DDI liability, a comprehensive illustration of DDI-related potencies is required by regulatory authorities as an essential part of in vitro toxicity profiles. Creative Biolabs has established a full portfolio of assay systems to provide our customers overall information concerning the DDI potential of investigated compounds.

Drug-Drug Interactions

CYP Investigations

Cytochrome 450 (CYP) is the key catalyzing enzyme during Phase I metabolism of most known drugs in human. Due to its diverse isoforms and broad substrate specificity, CYP has long been a major concern of DDI risks. Substances that exert inhibiting or inducing CYP properties need to be detected and eliminated in early development stage. Besides, to discover whether a compound is substrate of CYP and to find the specific isoform involved are also a critical part of predicting undesirable DDI.

Combined well-established in vitro expression model and elegant HPLC-MS/MS monitoring technology, our featured CYP investigation service includes:

  • CYP inhibition test
  • CYP induction test
  • CYP-reaction phenotyping assay

UGT Investigation

Uridine glucuronyl transferase (UGT) which is responsible for glucuronidation, plays a pivotal part in Phase II metabolic process of the bulk of drugs as well as biotransformation of many endogenous products like bilirubin. Therefore, early detection of inhibiting or inducing potency of drug compounds is of great significance.

Similar to CYP, we conduct UGT-focused investigations with highly tailored protocols to address customer issues:

  • UGT inhibition test
  • UGT induction test
  • UGT-reaction phenotyping assay

As an alternative, Creative Biolabs also offers investigation service of other drug enzymes, such as FMO, MAO, NAT, AOX, and CES.

Transporter Interactions

As an emerging area in recent years, transporter-mediated DDI is gaining increasing attention and heavily emphasized by FDA and EMA. Multiple transporters located on vast tissues and organs act a crucial role in drug absorption, distribution, and excretion. Functional disturbance of key transporters can lead to profound adverse effects. Currently, due to their multiplicity nature and function redundancy, efficient assessment of transporter-associated DDI is still faced with many challenges. With comprehensive knowledge and leading-edge in vitro technique platforms, Creative Biolabs provides first-class transporter interaction evaluating assays with extensive choices of uptake and efflux transporters.

We conduct both in vitro substrate assay (permeability ability of test article) and in vitro inhibition assay (permeability of probe substrate) using transporter-expressing monolayer or cell lines.

  • Caco2 Permeability Assay
  • Uptake Transporter Assay: OATPs (OATP1B1, OATP1B3), OCTs (OCT1, OCT2), OATs (OAT1, OAT3).
  • Efflux Transporter Assay: MDR1, MRP2, BCRP, BSEP, MATE1, MATE2-K.
  • Other transporter upon request.

Scientists in Creative Biolabs are glad to offer a one-stop solution of in vitro DDI assessment for subsequent decision-making and IND submission. For more detailed information, please feel free to contact us or directly sent us an inquiry.

For Research Use Only.



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