Regulatory Strategies
and Safety
Drug Metabolism and Pharmacokinetics

TriApex DMPK team is committed to providing pharmacokinetic research services for PK R&D studies at various research stages, including leading compound discovery and optimization, PCC identification, and other phases, to facilitate drug R&D from non-clinical to clinical stages.

Service Advantages

1.Comprehensive Research

Proficient in conducting various pharmacokinetic studies to support the development of new chemical entities (including siRNA) and biologics (including cellular & gene therapies).

Various animal species including non-human primate, dog, mini pig, mice (including tumor-bearing mice), rat, rabbit, guinea pig, golden hamsters.

2.Expertise in Various Drugs

New chemical entities (including oligonucleotides), antibodies, ADCs, cellular & gene therapies, etc.

3.Excellent Project Operation System

Certified standardized experimental system: high quality and high reproducibility of experimental data.

Professional project management system: high project operation efficiency and short operation cycle.

Service Capacities

1.Study on Physical and Chemical Properties

(1)Solubility study

(2)Lipophilicity study

(3)Solution stability study


(1)New Chemical Entities

Permeability study: Caco-2 cell model, MDR2-MDCK cell model

Absorption studies at one dose and multiple doses: rodent, non-rodent

Single dose and repeat dose absorption studies: rodent, non-rodent


Single dose and repeat dose absorption studies: rodent, non-rodent


(1)Chemical Entities

Blood plasma partition ratio: whole blood and plasma of various species

Plasma protein binding: equilibrium dialysis, ultrafiltration, electrophoretic mobility shift assay (EMSA)

Tissue distribution study: rodent

(2)Biologics/Cellular &Gene Therapies



(1)Metabolic stability study: liver microsome, liver S9, mixed liver cells of various species

(2)Metabolite identification study: metabolite identification in vitro and in vivo

(3)Metabolic phenotyping identification study: human liver microsome, recombinant human CYP450 isoenzyme (chemical inhibition method, recombinant enzyme method)

(4)UGT phenotyping identification


(1)Excretion study: bile, urine, feces

6.Drug-Drug Interaction

(1)Transporter study (substrates and inhibitors)

Efflux transporters: ABC transporter (P-gp, BCRP)

Uptake transporters: SLC transporter (OATP1B1, OATP1B3, OAT1, OATP3, OCT1, OCT3, MATE1, MATE2K)

(2)Metabolic enzyme inhibition study

CYP450 Isoform: 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4 and 2E1

(3)Metabolic enzyme induction study

CYP450 Isoform: CYP3A4, CYP2B6, CYP1A2

Project Experience

TriApex has successfully conducted more than 200 pharmacokinetic studies of new chemical entities (NCEs) and accelerated the development of these products.

Compound 1 is a small interfering RNA (siRNA) intended for the treatment of hyperlipidemia. We designed and conducted pharmacokinetic studies in vitro and in vivo to support IND application of the product. The studies are as follows:

Single dose pharmacokinetics study in rats and monkeys by subcutaneous injection

Study on tissue distribution in rats and plasma protein binding in vitro

Stability studies in serum and liver S9

Metabolite identification study in vitro and in vivo

CYP450 metabolic enzyme phenotyping study

Metabolic enzyme induction and inhibition study

Excretion study

Transporter study

The above studies fully demonstrated the pharmacokinetic characteristics of Compound 1, which facilitated IND application. The IND application has been approved.


1. Technical Guidelines for clinical Single and multiple dose escalation pharmacokinetic studies of chemotherapeutic innovative Drugs (No. 58 of 2021), NMPA, December 2021

2. Technical Guidelines for Clinical Pharmacology Research of Innovative Drugs (Draft), NMPA, August 2021

3. Technical Guidelines for Drug Interaction Studies (Pilot) (No. 4 of 2021), NMPA, Jan 2021

4. Technical Guidelines for Clinical pharmacokinetic Studies of Chemical Drugs, March 2005

5. FDA M9 Biopharmaceutics Classification System-Based Biowaivers, 2021.05

6. FDA In Vitro Drug Interaction Studies - Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions Guidance for Industry, 2020.01

7. ICH M10 Bioanalytical method validation and study sample analysis, 2023.01