^
7d
Evaluation of drug-drug interactions of a novel potent FLT3 inhibitor SKLB1028 in healthy subjects. (PubMed, Clin Transl Sci)
Based on the preclinical characterization of SKLB1028 metabolism, three drug-drug interaction clinical studies were performed to investigate the effects of itraconazole, rifampin (CYP3A4 inhibitor and inducer, respectively), and gemfibrozil (CYP2C8 inhibitor) on the metabolism of SKLB1028. Co-administration with rifampin reduced the AUC of SKLB1028 by ~30%, while the Cmax did not change significantly. All treatments were well tolerated in all three studies.
Journal
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FLT3 (Fms-related tyrosine kinase 3)
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FLT3-ITD mutation
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itraconazole • rifampicin • ruserontinib (SKLB-1028)
8d
P-RIF: Precision Rifampin Trial for Personalized Dosing (clinicaltrials.gov)
P1, N=200, Not yet recruiting, University of Virginia | Phase classification: P1/2 --> P1 | Initiation date: Jul 2024 --> Jan 2025
Phase classification • Trial initiation date
|
rifampicin
12d
A Single-center, Open-label, Fixed-sequence, Drug-Drug Interaction Study of BPI-16350 co-administered with Rifampin or Itraconazole in Healthy Volunteers (ChiCTR2400090190)
P1, N=36, Completed, Beijing Friendship Hospital ,Capital Medical University; Beijing Friendship Hospital ,Capital Medical University
New P1 trial
|
itraconazole • tibremciclib (BPI-16350) • rifampicin
16d
Evaluating the Early Bactericidal Activity, Safety and Tolerability of Nebulised RESP301 in Adults With Tuberculosis (clinicaltrials.gov)
P2, N=75, Active, not recruiting, Thirty Respiratory Limited | Recruiting --> Active, not recruiting | Trial primary completion date: Apr 2024 --> Apr 2025
Enrollment closed • Trial primary completion date
|
rifampicin
22d
Trial completion date • Metastases
|
TP53 (Tumor protein P53)
|
TP53 wild-type
|
brigimadlin (BI 907828) • itraconazole • rifampicin
24d
Abnormally high plasma concentrations of M-4, the active metabolite of edoxaban, at the onset of acute kidney injury in a patient receiving rifampin and clarithromycin: a case report. (PubMed, J Pharm Health Care Sci)
This case suggests that in patients with impaired renal function taking edoxaban, co-administration of carboxylesterase-1 inducers such as rifampin and/or OATP1B1 inhibitors such as rifampin or clarithromycin may increase plasma concentrations of M-4 to clinically non-negligible levels.
Journal
|
CES1 (Carboxylesterase 1)
|
rifampicin
24d
Drug-Drug Interaction (DDI) Study for TQB3616 (clinicaltrials.gov)
P1, N=40, Not yet recruiting, Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
New P1 trial
|
culmerciclib (TQB3616) • itraconazole • rifampicin
25d
New P1 trial
|
itraconazole • rifampicin
2ms
VA INTREPID: Investigation of Rifampin to Reduce Pedal Amputations for Osteomyelitis in Diabetics (clinicaltrials.gov)
P4, N=880, Recruiting, VA Office of Research and Development | Trial completion date: Sep 2024 --> Sep 2025 | Trial primary completion date: Sep 2024 --> Sep 2025
Trial completion date • Trial primary completion date
|
rifampicin
2ms
Early prediction and impact assessment of CYP3A4-related drug-drug interactions for small molecule anti-cancer drugs using human-CYP3A4-transgenic mouse models. (PubMed, Drug Metab Dispos)
Victim drugs brigatinib and lorlatinib were evaluated with the new approach in combination with the perpetrator drugs itraconazole and rifampicin. The model was able to adequately describe the inhibition of CYP3A4 metabolism and the subsequent magnitude of change in exposure. However, it was unable to accurately predict the magnitude of change in exposure of victim drugs in combination with an inducer.
Preclinical • Journal
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CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
|
Lorbrena (lorlatinib) • Alunbrig (brigatinib) • itraconazole • rifampicin
2ms
New P1 trial
|
itraconazole • VC004 • rifampicin
2ms
Trial completion
|
itraconazole • golcadomide (CC-99282) • rifampicin
2ms
ASTERoiD: Assessment of the Safety, Tolerability, and Effectiveness of Rifapentine Given Daily for LTBI (clinicaltrials.gov)
P2/3, N=3400, Recruiting, Centers for Disease Control and Prevention | Trial completion date: Dec 2028 --> Dec 2029 | Trial primary completion date: Dec 2028 --> Dec 2029
Trial completion date • Trial primary completion date
|
CD4 (CD4 Molecule)
|
rifampicin
2ms
New trial
|
rifampicin
3ms
Pharmacokinetics of olverembatinib (HQP1351) in the presence of a strong CYP3A4 inhibitor (itraconazole) or inducer (rifampin) in healthy volunteers. (PubMed, Clin Transl Sci)
Coadministration with rifampin decreased these same variables by 61.27%, 74.21%, and 75.19%, respectively. These results confirm that olverembatinib is primarily metabolized by CYP3A4 in humans, suggesting that caution should be exercised with concurrent use of olverembatinib and strong CYP3A4 inhibitors or inducers.
PK/PD data • Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
ABL1 T315I
|
Nailike (olverembatinib) • itraconazole • rifampicin
3ms
Building Evidence for Advancing New Treatment for Rifampicin Resistant Tuberculosis (RR-TB) Comparing a Short Course of Treatment (Containing Bedaquiline, Delamanid and Linezolid) With the Current South African Standard of Care (clinicaltrials.gov)
P3, N=402, Completed, Wits Health Consortium (Pty) Ltd | Active, not recruiting --> Completed | Trial completion date: Jun 2023 --> Apr 2024 | Trial primary completion date: Jun 2023 --> Apr 2024
Trial completion • Trial completion date • Trial primary completion date
|
rifampicin
3ms
Pregnane X receptor inhibits the transdifferentiation of hepatic stellate cells by downregulating periostin expression. (PubMed, Biochem J)
This induction was attenuated upon PXR activation in hPXR-LX2 cells by treatment with the destabilization domain-stabilizing chemical Shield-1 and the human PXR ligand rifampicin...Reporter assays with the POSTN promoter showed that PXR inhibited the NF-κB-mediated transcription of POSTN. Consequently, PXR activation in HSCs is expected to inhibit transdifferentiation by downregulating POSTN expression, thereby suppressing EMT of liver cancer cells.
Journal
|
TGFB1 (Transforming Growth Factor Beta 1) • COL1A1 (Collagen Type I Alpha 1 Chain) • POSTN (Periostin)
|
rifampicin
3ms
CONTRol-TB: French National Cohort of Patients With Rifampicin-Resistant Tuberculosis (clinicaltrials.gov)
P=N/A, N=300, Not yet recruiting, Assistance Publique - Hôpitaux de Paris
New trial
|
rifampicin
3ms
Correlations of LncRNA HNF4A-AS1 Alternative Transcripts with Liver Diseases and Drug Metabolism. (PubMed, Drug Metab Dispos)
The expression patterns of all HNF4A-AS1 transcripts were further investigated in liver cell growth from human embryonic stem cells to matured hepatocyte-like cells, HepaRG differentiation, and exposure to rifampicin treatment...Significance Statement This study explores the alternative transcripts of HNF4A-AS1, showing how their expression changes in different biological conditions, from various liver diseases to the growth and differentiation of hepatocytes, and drug metabolism. The generated knowledge is essential for understanding the independent roles of different transcripts from the same lncRNA in different liver diseases and drug metabolism situations.
Journal
|
CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • HNF1A (HNF1 Homeobox A)
|
rifampicin
3ms
A Drug-Drug Interaction (DDI) Study of HDM1002 With Rifampicin and Itraconazole in Healthy Subjects (clinicaltrials.gov)
P1, N=40, Not yet recruiting, Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd.
New P1 trial
|
itraconazole • rifampicin
3ms
Co-SAM: An Adaptive Multi-arm Trial to Improve Clinical Outcomes Among Children Recovering From Complicated SAM (clinicaltrials.gov)
P3, N=1266, Recruiting, Queen Mary University of London | Not yet recruiting --> Recruiting
Enrollment open
|
CCL2 (Chemokine (C-C motif) ligand 2)
|
rifampicin
3ms
A Clinical Trial to Evaluate the Effect of Itraconazole and Rifampicin on ABSK021 (clinicaltrials.gov)
P1, N=32, Completed, Abbisko Therapeutics Co, Ltd | Enrolling by invitation --> Completed | Trial completion date: Nov 2023 --> Sep 2023
Trial completion • Trial completion date
|
itraconazole • pimicotinib (ABSK021) • rifampicin
4ms
RICHH: Rifampin in CYP24A1-related Hypercalcemia and Hypercalciuria (clinicaltrials.gov)
P2, N=60, Recruiting, Children's Hospital of Philadelphia | N=30 --> 60
Enrollment change
|
rifampicin
4ms
Predict the Drug-Drug Interaction of a Novel PI3Kα/δ Inhibitor, TQ-B3525, and Its Two Metabolites Using Physiologically Based Pharmacokinetic Modeling. (PubMed, J Clin Pharmacol)
Models involving rifampicin combined with midazolam, itraconazole combined with midazolam or digoxin were utilized to showcase the robustness of evaluating DDI effects. PBPK model simulation results showed that the systemic exposure of TQ-B3525 was significantly affected when co-administered with CYP3A4/P-gp inducers and inhibitors. This indicates that the combination with strong inducers and inhibitors should be carefully avoided or adjust the dosage of TQ-B3525 in clinic.
PK/PD data • Journal
|
PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
|
itraconazole • TQ-B3525 • midazolam hydrochloride • rifampicin
4ms
A Short Regimen for Rifampicin-resistant Isoniazid-susceptible TB (clinicaltrials.gov)
P3, N=100, Not yet recruiting, Taipei Medical University WanFang Hospital
New P3 trial
|
rifampicin
4ms
Effect of Efavirenz on the Pharmacokinetics of SHR6390 in Healthy Volunteers. (PubMed, Drug Des Devel Ther)
Previous studies have shown that SHR6390 in combination with rifampicin, a potent inducer of CYP3A4, significantly reduces exposure levels. It is recommended to avoid concomitant administration of moderate inducers of CYP3A4 during treatment with SHR6390. http://www.chinadrugtrials.org.cn/index.html, CTR20211571/ https://classic.clinicaltrials.gov, NCT04973020.
Clinical • PK/PD data • Journal
|
CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
|
AiRuiKang (dalpiciclib) • efavirenz • rifampicin
4ms
Rifampicin Resistance in S. Aureus During and After Treatment for Latent Tuberculosis (clinicaltrials.gov)
P=N/A, N=100, Recruiting, Region Skane | Trial completion date: Dec 2024 --> Dec 2026 | Trial primary completion date: Jun 2024 --> Dec 2026
Trial completion date • Trial primary completion date
|
rifampicin
4ms
An Adaptive Trial to Find the Safest And Shortest TB Preventive Regimens. (clinicaltrials.gov)
P2/3, N=1800, Not yet recruiting, McGill University Health Centre/Research Institute of the McGill University Health Centre
New P2/3 trial
|
rifampicin
4ms
New P3 trial
|
rifampicin
5ms
New P1 trial
|
Ensacove (ensartinib) • itraconazole • rifampicin
5ms
New P3 trial • Head-to-Head
|
rifampicin
5ms
Recurrent rejections after liver transplantation for hepatocellular carcinoma with stem cell features in an adult patient. (PubMed, Acta Clin Belg)
Despite being on conventional immunosuppressive regimens (tacrolimus and mycophenolate mofetil with initial corticosteroids tapered), this patient still developed two severe rejection episodes, one of which necessitated retransplantation (DCD). Both episodes were preceded by alterations in tacrolimus trough levels, either intentionally, when tacrolimus was reduced within a nephroprotective regimen, or unintentionally, when rifampicin, a CYP3A4 inducer, significantly lowered the trough levels...Furthermore, the patient experienced an everolimus-linked drug-induced thrombotic microangiopathy, underwent multiple ERCPs for an anastomotic stricture and only one and a half year after the first liver transplantation she already suffers from long-term immunosuppressive-related side effects such as impaired glucose tolerance, hypertension and a potential cardiomyopathy. At present, she is still alive and experienced no recurrence of her primary tumor. Her case underscores the significant challenges in post-liver transplantation care.
Journal
|
CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
|
everolimus • rifampicin
5ms
Enrollment closed • Metastases
|
TP53 (Tumor protein P53)
|
brigimadlin (BI 907828) • itraconazole • rifampicin
5ms
Co-SAM: An Adaptive Multi-arm Trial to Improve Clinical Outcomes Among Children Recovering From Complicated SAM (clinicaltrials.gov)
P3, N=1266, Not yet recruiting, Queen Mary University of London | Initiation date: Mar 2024 --> Jul 2024 | Trial primary completion date: Mar 2026 --> Jul 2026
Trial initiation date • Trial primary completion date
|
CCL2 (Chemokine (C-C motif) ligand 2)
|
rifampicin
5ms
Concomitant osimertinib and antituberculosis therapy in an elderly patient with EGFR-mutated lung cancer and pulmonary tuberculosis: A case report. (PubMed, Thorac Cancer)
We report a case of successful treatment involving the concomitant administration of osimertinib and antituberculosis drugs in an older patient, an 89-year-old female, diagnosed with epidermal growth factor receptor (EGFR)-mutant lung cancer and pulmonary tuberculosis. Accumulating evidence is warranted to develop an optimal treatment strategy for patients with lung cancer and tuberculosis.
Clinical • Observational data • Retrospective data • Review • Journal
|
EGFR (Epidermal growth factor receptor)
|
Tagrisso (osimertinib) • rifampicin
5ms
A Clinical Trial to Evaluate JAB-21822 Drug-drug Interactions in Healthy Subjects (clinicaltrials.gov)
P1, N=66, Completed, Jacobio Pharmaceuticals Co., Ltd. | Recruiting --> Completed | Trial completion date: Jul 2024 --> Feb 2024 | Trial primary completion date: Jun 2024 --> Feb 2024
Trial completion • Trial completion date • Trial primary completion date
|
glecirasib (JAB-21822) • itraconazole • midazolam hydrochloride • omeprazole • rifampicin
6ms
New P3 trial
|
rifampicin
6ms
Integrated PBPK-EO modeling of osimertinib to predict plasma concentrations and intracranial EGFR engagement in patients with brain metastases. (PubMed, Sci Rep)
The purpose of this study was to develop and validate a physiologically based pharmacokinetic (PBPK) model combined with an EGFR occupancy (EO) model for osimertinib (OSI) to predict plasma trough concentration (Ctrough) and the intracranial time-course of EGFR (T790M and L858R mutants) engagement in patient populations. When used concomitantly with CYP enzyme perpetrators, the PBPK-EO model suggested appropriate dosing regimens of 80 mg OD with fluvoxamine (FLUV) itraconazole (ITR) or fluvoxamine (FLUC) for co-administration and an increase to 160 mg OD with rifampicin (RIF) or efavirenz (EFA). In conclusion, the PBPK-EO model has been shown to be capable of simulating the pharmacokinetic concentration-time profiles and the time-course of EGFR engagement for OSI, as well as determining the optimum dosing in various clinical situations.
Journal
|
EGFR (Epidermal growth factor receptor) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
|
Tagrisso (osimertinib) • itraconazole • efavirenz • rifampicin
6ms
Specific human CYP enzymes-dependent mutagenicity of tris(2-butoxyethyl) phosphate (an organophosphorus flame retardant) in human and hamster cell lines. (PubMed, Chem Biol Interact)
In C3A cells (endogenous CYPs being substantial), TBOEP exposing for 72 h (2-cell cycle) at low micromolar levels induced micronucleus, which was abolished by 1-aminobenzotriazole (inhibitor of CYPs); in HepG2 cells (CYPs being insufficient) TBOEP did not induce micronucleus, whose effect was however potentiated by pretreating the cells with PCB126 (CYP1A1 inducer) or rifampicin (CYP3A4 inducer)...In C3A cells, TBOEP selectively induced centromere protein B-free micronucleus (visualized by immunofluorescence) and PIG-A gene mutations, and elevated γ-H2AX rather than p-H3 (by Western blot), indicating double-strand DNA breaks. Therefore, this study suggests that TBOEP may induce DNA/chromosome breaks and gene mutations in human cells, which requires metabolic activation by CYPs, primarily CYP1A1 and 3A4.
Preclinical • Journal
|
CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • CYP1A1 (Cytochrome P450 Family 1 Subfamily A Member 1)
|
rifampicin