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Prior to opt-in by AbbVie, Hotspot Therapeutics and AbbVie will be responsible for design of the FIH study (SAD/MAD in HVs); Hotspot Therapeutics will be responsible for the conduct of the SAD and MAD studies in healthy volunteers (HV).
3. Preparation for submission of IND/CTA
Prior to opt-in by AbbVie, Hotspot Therapeutics will be responsible for submission of an IND or CTA to conduct the FIH study (SAD/MAD in HVs). After opt-in by AbbVie, Hotspot Therapeutics will transfer sponsor responsibilities for the IND or CTA to AbbVie and AbbVie will become responsible for the IND.
CLINICAL DEVELOPMENT PLAN
A. Plan for SAD and MAD Phase I Clinical Trial
All clinical activities are the responsibility of HotSpot Therapeutics unless otherwise noted below.
The following are the Clinical Studies contemplated by the Parties for successful Development of Hotspot Therapeutics's IRF5 compound for the treatment of SLE through the end of the Phase I MAD.
A placebo-controlled, double-blind randomized single ascending dose (SAD) Clinical Trial of Hotspot Therapeutics's IRF5 compound in adult healthy volunteers (18-65 years old) will be conducted. The SAD Clinical Study will assess the safety, tolerability, pharmacokinetics, pharmacodynamics of single oral dose of Hotspot...
The placebo-controlled, double-blind randomized multiple ascending dose (MAD) Clinical Trial is a dose escalation study that would assess the safety, tolerability, pharmacokinetics, pharmacodynamics of multiple oral doses of Hotspot Therapeutics's IRF5 compound in adult healthy volunteers (18-65 years old). It is antic...
Figure 1. Phase I SAD/MAD Clinical Study Design Scheme
[Note: Figure not included in text extraction]
Table 5. Phase 1 Clinical Plan Activities
Clinical Objectives (Responsibility Hotspot Therapeutics)
SAD Phase 1 Clinical Trial in Healthy Volunteers (HV)
MAD Phase 1 Clinical Trial in HV
B. Development of Pharmacodynamic (PD) Markers to End of Phase 1 Clinical Trial
Activities to support development of PD markers are outlined in the Table 6 below:
Table 6. Development of PD Biomarkers
Translational Medicine / Biomarker Objectives
Develop and validate target engagement (TE) and PD biomarker
Evaluation of exploratory biomarkers
GMP material synthesis
GMP drug product and placebo sufficient to support the first Phase 1b study of the Licensed Product in the first indication and the first Phase 2 study of the Licensed Product in the first indication will be manufactured by Hotspot Therapeutics and delivered to AbbVie in accordance with Section 3.8 of the Agreement, as...
Final Data Package Deliverables:
After completing all of the activities set forth in this Development Plan and Budget, Hotspot Therapeutics will provide a complete data package containing all data, findings, information and results of the development and CMC activities set forth in this Development Plan and Budget and all supporting documentation (inc...
a) all Information Reports (to the extent not previously provided)
b) top line data from the 13-week GLP toxicology studies (including histopathology data and slides)
c) top line results and patient level data for the first single ascending dose Phase I Study sponsored by HotSpot Therapeutics compliant with ICH E3 guidelines, and;
d) top line results, and if available prior to the Final License Option Expiration Date the complete study report, and patient level data for the first multiple ascending dose Phase I Study sponsored by HotSpot Therapeutics compliant with ICH E3 guidelines
Budget and Minimal Hotspot Therapeutics FTEs
The table below represents the budget required (by expense category) to complete each deliverable detailed in this proposal.
[Table with budget details]
FTEs
Stage 1
Stage 2
Stage 3
Stage 4
FUNCTIONAL AREA
Medicinal chemistry
Biology (in vitro)
Pharmacology (in vivo)
Development Sciences (ADME/PK, Tox & Clin Pharm)
Translational Biology
CMC
Clinical
Operations
TOTAL
APPENDICES
Appendix A: Product-Specific In Vitro Cellular Assays and In Vivo Acute and Chronic Models for Advancement of IRF5 Research Target
Attribute
Effects of test compound should be comparable to or superior to listed standards in each of the following assays or models
In Vitro Screening Assay in addition to Hotspot Therapeutics protein assay for chemical matter identification
IRF5 dimerization assay
WT Thp1 R848 Assay
IRF5 KO Thp1 Pam3 Assay
IRF5 Binding
In Vitro Assays to understand mechanism of action
Biophysical assays
Cellular functional assay
Cellular functional assay
IRF5 nuclear translocation
Whole blood assay
In Vivo Acute Efficacy
Acute TLR agonist R848 model
Short term efficacy model:
In Vivo Chronic Efficacy Model
SLE efficacy model
Appendix B: CMC Workplan (at time of initiation of collaboration)
Hotspot Therapeutics/AbbVie CMC Workplan (Pre-IND Activities/Deliverables)
Deliverable
Stage 2 Support
Stage 3 support
Stage 3/4 support
Stage 4 and Clinical Development Support
Deliverable
OPT-IN Activity Description
Documentation of drug substance and drug product development in respective development reports (identification, structural confirmation, process development, analytical development, control strategy, reference standard, stability)
Transfer DS/DP analytical methods by: • Providing written methods for all analytical release and stability assays for non-USP methods which support regulatory filings • Formal transfer methods of product specific methods are required
Provide consultation to answer questions regarding analytic methods
Setup contracts with DS/DP CDMOs conducting stability studies to transfer control of studies to AbbVie
Continue to provide storage of DS/DP GMP stability samples and regulatory retains or coordinate transfer to site determined by AbbVie
Provide DS/DP release and stability testing of new GMP/clinical lots until transfer of stability studies is complete
Assume control and costs for DS/DP stability studies and storage of materials
Hotspot Therapeutics DS/DP materials to be shipped to site TBD by AbbVie at the completion of tech transfer, except for materials needed to complete tech transfer, such as reference standards: • List materials • DS/DP inventory (SM, INT, DS, DP) • Reference standards • Samples in support of tech transfer or manufacturi...
Note: Inventory may remain at current suppliers until contracts with AbbVie are in place. Material requests will be facilitated by the Hotspot Therapeutics team.
Provide DS/DP reports which support technology transfer including: • developmental history reports • technical development reports • Executed batch records • CoA's and supporting analytical data • Reports that support CMC section of the IND/CTD • GMP CDMO audit reports and quality agreements
Provide documentation/communications with Regulatory Agencies
DS/DP Tech transfer Process • Coordinate 3-way CDAs with mfg. vendors • Setup F2F meetings at mfg. sites • Provide tech transfer support to manufacturing sites of AbbVie's choosing
Drug Product Deliverable
Drug Product • GMP drug product sufficient to support the first Phase 1b and Phase 2 study of the Licensed Product in the first indication • Placebo sufficient to support the first Phase 1b and Phase 2 study of the Licensed Product in the first indication
Appendix C: Nonclinical and CMC reports and documents to be included for an IND
submission
Nonclinical reports for an IND (small molecule) should cover, but not limited to, the following topics:
Pharmacology
● Primary Pharmacology: in vitro, in vivo
● Secondary Pharmacology: off target binding assays for receptors, ion channels, enzymes and transporters
● Safety Pharmacology: CV (hERG, in vivo), CNS, respiratory
Pharmacokinetics
● Bioanalytical method validation
● Absorption: cellular permeability, pharmacokinetics in nonclinical species, dose response, formulation effects (if necessary)