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Poziotinib

Phase 2

Breast Cancer | Small molecule | Oncology |Assertio Holdings, Inc.|Last Updated: Mar 11, 2022

Success Probability

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Market & Valuation

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Trial Design

CONTROLLEDBiomarker
Total Trials1
Total Enrollment67

FDA Designations

No designations recorded

Clinical trial landscape

Poziotinib · 3 trials · 2 indications

Phase 2 1Phase 1 2
NCT02659514Study of Poziotinib in Participants With HER2-Positive Metastatic Breast CancerBreast Cancer
COMPLETED67 Analytics
PHASE2COMPLETED
Study of Poziotinib in Participants With HER2-Positive Metastatic Breast Cancer
Breast CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Objective Response Rate (ORR)
Up to 24 months

ORR was defined as the percentage of participants whose best overall response (BOR) was complete response (CR) or partial response (PR) among participants in the Evaluable Population assessed per Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST v1.1). ORR was based on investigator assessed BOR. Per RECIST v1.1 for target lesions, CR was disappearance of all target tumor lesions (TLs) and all target lymph nodes (LNs) with short axis \<10mm. PR was ≥30% decrease in sum of diameters (SOD) from Baseline, and not progressive disease (PD) (≥20% increase in SOD from previous smallest SOD on study, and an absolute increase of ≥5mm).

Area Under the Curve (AUC) of Poziotinib and Metabolites (M1 and M2) Following Poziotinib Administrations With and Without Itraconazole [Part 1], Phenytoin [Part 2], or Paroxetine [Part 3]
Part 1 and Part 3, predose and up to 120 hours postdose; Part 2, predose and up to 96 hours postdose
Maximum Observed Concentration (Cmax) of Poziotinib and Metabolites (M1 and M2) Following Poziotinib Administration With and Without Itraconazole [Part 1], Phenytoin [Part 2], or Paroxetine [Part 3]
Part 1 and Part 3, predose and up to 120 hours postdose; Part 2, predose and up to 96 hours postdose
Apparent Clearance (CL/F) of Poziotinib Following Poziotinib Administration With and Without Itraconazole [Part 1], Phenytoin [Part 2], or Paroxetine [Part 3]
Part 1 and Part 3, predose and up to 120 hours postdose; Part 2, predose and up to 96 hours postdose
Time to Maximum Observed Concentration (Tmax) for Poziotinib and Metabolites (M1 and M2) Following Poziotinib Administration With and Without Itraconazole [Part 1], Phenytoin [Part 2], or Paroxetine [Part 3]
Part 1 and Part 3, predose and up to 120 hours postdose; Part 2, predose and up to 96 hours postdose
Maximum Observed Plasma Concentration (Cmax) of [14C]-Poziotinib, Metabolites M1 and M2
1-15 days
Cmax of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
1-15 days
Time to Attain Maximum Observed Plasma Concentration (Tmax) of [14C]-Poziotinib, Metabolites M1 and M2
1-15 days
Tmax of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
1-15 days
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC[last]) of [14C]-Poziotinib, Metabolites M1 and M2
1-15 days
AUC(last) of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
1-15 days
Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUCinf) of [14C]-Poziotinib, Metabolites M1 and M2
1-15 days
AUC(inf) of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
1-15 days
Percentage of AUCinf Derived by Extrapolation (%AUCext) of [14C]-Poziotinib, Metabolites M1 and M2
1-15 days
%AUCext of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
1-15 days
Apparent Terminal Elimination Half-Life (t1/2) of [14C]-Poziotinib, Metabolites M1 and M2
1-15 days
t1/2 of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
1-15 days
Elimination Rate Constant (λz, or kel) of [14C]-Poziotinib, Metabolites M1 and M2
1-15 days
λz, or kel of Total Radioactivity of [14C]-Poziotinib in Whole Blood and Plasma
1-15 days
Apparent Volume of Distribution (VZ/F) During Terminal Phase of [14C]-Poziotinib
1-15 days
Apparent Oral Clearance (CL/F) of [14C]-Poziotinib
1-15 days
Whole Blood : Plasma Concentration Ratios of Total Radioactivity of [14C]-Poziotinib
1-15 days
Total Radioactivity of Cumulative Amount Excreted in Urine (Aeu)
1-15 days
Total Radioactivity of Fraction of Dose Excreted in Urine (feu)
1-15 days
Total Radioactivity of Cumulative Amount Excreted in Feces (Aef)
1-15 days
Total Radioactivity of Fraction of Dose Excreted in Feces (fef)
1-15 days
Total Radioactivity of Cumulative Total Amount Excreted (Aetotal)
1-15 days
Total Radioactivity of Fraction of Dose Excreted in Urine and Feces (fetotal)
1-15 days
Poziotinib Metabolite Profiling and Identification in Plasma
1-15 days

Secondary Endpoints

Progression Free Survival (PFS)
Up to 24 Months
Disease Control Rate (DCR)
Up to 24 months
Time to Progression (TTP)
Up to 24 months
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSEQUENTIAL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Cohort 1: Poziotinib 24 mgEXPERIMENTALParticipants received poziotinib 24 milligrams (mg), administered as three 8 mg tablets, orally, once daily (QD) on an intermittent dosing schedule of 14 days on treatment followed by 7 days off treatment, in a 21-day cycle until disease progression, death, intolerable adverse events (AEs) or for up to a maximum of 24 months, whichever occurs first.
Cohort 2: Poziotinib 16 mgEXPERIMENTALParticipants received poziotinib 16 mg, administered as two 8 mg tablets, orally, QD, on a continuous dosing schedule in a 21-day cycle until disease progression, death, intolerable AEs or for up to a maximum of 24 months, whichever occurs first.
Part 1: Itraconazole/Poziotinib Drug-drug interaction (DDI)EXPERIMENTALOn Day 1 of Treatment period 1, a single oral dose of 8 milligrams (mg) poziotinib will be administered. On Day 1 of Treatment Period 2, 200 mg itraconazole oral solution will be administered twice a day (BID) followed by 200 mg itraconazole oral solution once daily (QD) for 7 consecutive days (Day 2 to Day 8) with a single oral dose of 8 mg poziotinib coadministered on Day 4.
Part 2: Phenytoin/Poziotinib DDIEXPERIMENTALOn Day 1 of Treatment period 1, a single oral dose of 16 mg poziotinib will be administered. In treatment period 2, an oral dose of 100 mg phenytoin will be administered three times daily (TID) for 17 consecutive days (Day 1 to Day 17) with a single oral dose of 16 mg poziotinib coadministered on Day 14.
Part 3: Paroxetine/Poziotinib DDIEXPERIMENTALOn Day 1 of Treatment Period 1, a single oral dose of 8 mg poziotinib will be administered. On Day 1 and Day 2 of Treatment Period 2, an oral dose of 20 mg paroxetine will be administered BID followed by 20 mg paroxetine QD for 9 consecutive days (Day 3 to Day 11) with a single oral dose of 8 mg poziotinib coadministered on Day 7.
PoziotinibEXPERIMENTALA single oral dose of 8 mg poziotinib as a capsule formulation (as the hydrochloride salt) containing approximately 100 μCi of \[14C\]-poziotinib

Interventions

NameTypeDescription
PoziotinibDRUG8 mg oral tablets, administered QD.
ItraconazoleDRUGItraconazole Oral solution
PhenytoinDRUGPhenytoin Capsules
ParoxetineDRUGParoxetine Tablets
[14C]-PoziotinibDRUGSingle oral administration of 8 mg (as the hydrocholoride salt) of \[14C\]-poziotinib
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Eligibility Criteria

Age Range18 Years to 90 Years
SexALL
Healthy VolunteersNo
Study Sites35

Inclusion Criteria: 1. Histopathologically confirmed primary breast cancer with metastatic lesions. 2. Confirmed HER2 overexpression or gene-amplified tumor 3. At least two prior HER2-directed therapy regimens for breast cancer, including trastuzumab and trastuzumab emtansine 4. Measurable disease ...

Countries:United States
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Competitive Landscape -Breast Cancer 402 trials

Top 20 of 92 competitors

CompanyTickerTrialsLead PhaseDrugs
AstraZeneca PLCAZN47PHASE3Fulvestrant, Capivasertib
Merck & Co., Inc.MRK12PHASE3Pembrolizumab, Paclitaxel, Doxorubicin, Epirubicin, Cyclophosphamide
Eli Lilly and CompanyLLY27PHASE3Abemaciclib, Standard Adjuvant Endocrine Therapy
BioNTech SE Sponsored ADRBNTX7PHASE3DB-1303/BNT323, T-DM1
Gilead Sciences, Inc.GILD13PHASE3Sacituzumab Govitecan-hziy, Eribulin, Capecitabine Product, Gemcitabine, Vinorelbine
Novartis AG Sponsored ADRNVS30PHASE3Ribociclib
Pfizer Inc.PFE34PHASE3ARV-471, Fulvestrant
BeOne Medicines Ltd. Sponsored ADRONC5PHASE3BGB-43395, Letrozole, Abemaciclib, Palbociclib, Ribociclib
Olema Pharmaceuticals, Inc.OLMA5PHASE3Palazestrant, Fulvestrant, Anastrozole, Letrozole, Exemestane
Jazz Pharmaceuticals Public Limited CompanyJAZZ3PHASE3Zanidatamab, Trastuzumab, Eribulin, Vinorelbine, Gemcitabine
Celcuity Inc.CELC3PHASE3Gedatolisib, Palbociclib, Fulvestrant, Alpelisib
Relay Therapeutics, Inc.RLAY2PHASE3Zovegalisib, Capivasertib, Fulvestrant
GSK plc Sponsored ADRGSK2PHASE3Niraparib
Greenwich LifeSciences, Inc.GLSI1PHASE3GLSI-100
Bristol-Myers Squibb CompanyBMY5PHASE2Iza-bren, Nab-paclitaxel, Paclitaxel, Capecitabine, Carboplatin
BriaCell Therapeutics CorpBCTX2PHASE3SV-BR-1-GM, Cyclophosphamide, Interferon infiltration of the inoculation site, Retifanlimab, Treatment of Physician's Choice
Incyte CorporationINCY4PHASE2Ruxolitinib, Capecitabine, Regorafenib
Natera, Inc.NTRA3PHASE2Discontinuation of the anti-HER2 maintenance therapy
Puma Biotechnology, Inc.PBYI3PHASE2Neratinib, Loperamide, Colesevelam
Atossa Therapeutics, Inc.ATOS1PHASE2endoxifen, goserelin
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Frequently asked questions about Poziotinib

What is Poziotinib used for?

Poziotinib is an investigational small molecule being studied for the treatment of HER2-positive metastatic breast cancer. It is also being evaluated in healthy subjects for pharmacokinetic studies. The drug is currently in Phase 2 clinical development for breast cancer, with completed trials in this indication.

What does Poziotinib target?

Poziotinib targets HER2, a protein that can promote cancer cell growth. It is being studied in patients with HER2-positive metastatic breast cancer, where this target is overexpressed. The drug is designed to inhibit HER2 signaling, potentially slowing tumor progression in this patient population.

Who makes Poziotinib?

Poziotinib is being developed by Assertio Holdings, Inc., a company traded on NASDAQ under the ticker symbol ASRT. The company is conducting clinical trials to evaluate the drug's safety and efficacy in oncology and healthy volunteer studies.

What phase is Poziotinib in?

Poziotinib is in Phase 2 clinical development for HER2-positive metastatic breast cancer. It has completed two clinical trials, including a Phase 2 study in breast cancer and a Phase 1 study in healthy subjects. The drug is investigational and not yet approved by regulatory authorities.

What clinical trials is Poziotinib in?

Poziotinib has completed two clinical trials. NCT02659514 was a Phase 2 study in 67 patients with HER2-positive metastatic breast cancer in the United States. NCT04436562 was a Phase 1 study in 8 healthy male subjects to evaluate absorption, metabolism, and excretion of the drug.

Is Poziotinib the same as any other drug?

Poziotinib is not known by any alternative names. It is being developed under this single name by Assertio Holdings, Inc. for the treatment of HER2-positive metastatic breast cancer and for pharmacokinetic studies in healthy volunteers.