Lantheus Strategic Investment and Capital Raise Presentation
Released
Released
Announcement PDF
Lantheus Strategic Investment and Capital Raising
June 2024
Not for release to US wire services or distribution in the United
R A DIO States
P H A R M TH E R A N O STIC S L TD 20 24
1
IMPORTANT NOTICE AND DISCLAIMER
The information in this presentation does not constitute personal investment advice. The presentation is not intended to be comprehensive or provide all information required
by investors to make an informed decision on any investment in Radiopharm Theranostics Ltd ACN 647 877 889 (Company). In preparing this presentation, the Company did
not take into account the investment objectives, financial situation and particular needs of any particular investor. Further advice should be obtained from a professional
investment adviser before taking any action on any information dealt with in the presentation. Those acting upon any information without advice do so entirely at their own
risk.
Whilst this presentation is based on information from sources which are considered reliable, no representation or warranty, express or implied, is made or given by or on behalf
of the Company, any of its directors, or any other person about the accuracy, completeness or fairness of the information or opinions contained in this presentation. No
responsibility or liability is accepted by any of them for that information or those opinions or for any errors, omissions, misstatements (negligent or otherwise) or for any
communication written or otherwise, contained or referred to in this presentation. Neither the Company nor any of its directors, officers, employees, advisers, associated
persons or subsidiaries are liable for any direct, indirect or consequential loss or damage suffered by any person as a result of relying upon any statement in this presentation
or any document supplied with this presentation, or by any future communications in connection with those documents and all of those losses and damages are expressly
disclaimed.
Certain statements contained in this presentation, including, without limitation, statements containing the words “believes,” “plans,” “expects,” “anticipates,” and words of
similar import, constitute “forward-looking statements.” Such forward-looking statements involve known and unknown risks, uncertainties and other factors that may cause
the actual results, performance or achievements of the Company to be materially different from any future results, performance or achievements expressed or implied by such
forward-looking statements. Such factors include, among others, the following: the risk that our clinical trials will be delayed and not completed on a timely basis; the risk that
the results from the clinical trials are not as favourable as we anticipate; the risk that our clinical trials will be more costly than anticipated; and the risk that applicable
regulatory authorities may ask for additional data, information or studies to be completed or provided prior to their approval of our products. Given these uncertainties, undue
reliance should not be placed on such forward-looking statements. The Company disclaims any obligation to update any such factors or to publicly announce the results of
any revisions to any of the forward-looking statements contained herein to reflect future events or developments except as required by law.
This presentation is not a prospectus or other disclosure document under the Corporations Act 2001 (Cth) and will not be lodged with the Australian Securities and
Investments Commission. This presentation is for information purposes only and is not an invitation or offer of securities for subscription, purchase or sale in any jurisdiction.
The distribution of this presentation (including electronically) outside Australia may be restricted by law. If you come into possession of this presentation, you should observe
such restrictions as any non-compliance with these restrictions could contravene applicable securities laws (see the section captioned ‘Foreign offer restrictions’). In particular,
this document does not constitute an offer to sell, or a solicitation of an offer to buy, securities in the United States. The new shares, the options and the ordinary shares
underlying the options have not been, and will not be, registered under the US Securities Act of 1933 and may not be offered or sold in the United States except in transactions
exempt from, or not subject to, the registration requirements of the US Securities Act and applicable US state securities laws.
Any opinions expressed reflect the Company’s position at the date of this presentation and are subject to change.
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD IS AT THE CUTTING EDGE OF RADIOPHARMACEUTICALS,
A TRANSFORMATIVE MODALITY WITHIN CANCER TREATMENT
1
Differentiated Within Radiopharmaceuticals
•
Clinical-stage company with deep pipeline of radiotherapeutic assets pursuing novel targets, leveraging insights from ADCs, using innovative targeting
moieties such as nanobodies
–
–
2
3
4
5
Targets include PD-L1, HER2, TROP2 (nanobody platform); integrin αVβ6 (peptide) fatty acid synthase (small molecule)
Preclinical technologies (mAb-based)
Radiopharm Ventures, a Joint Venture with MD Anderson Cancer Center
•
•
JV (private company) in-licensed from MDACC technologies for radiopharmaceuticals use
First technology has been disclosed (B7H3-targeting molecule)
Radiopharmaceuticals Expertise, In licensing Strategy & Intellectual Property
•
•
•
•
All team members with previous imaging and therapeutic radiopharmaceutical experience
Extensive Scientific Advisory Board of accredited multinational researchers
Proprietary molecules designed to identify and target a broad range of malignancies in solid tumors
Extensive patent portfolio for targets through 2040
Lantheus Strategic Investment
•
Lantheus Omega, LLC, a wholly owned subsidiary of Lantheus Holdings, Inc (LNTH.NASDAQ, Market Cap approximately US$5.5Bn) (Lantheus) has entered into
agreement with Radiopharm to invest, subject to shareholder approval, ~A$7.5m. Shares to be acquired at A$0.05, which represents a ~47% premium to the
last closing price on 19 June 2024 and a ~57% premium to the 5-day VWAP. Option to invest a further ~A$7.5m within 6 months
•
Under a separate agreement, Lantheus will also secure rights over two early preclinical assets in exchange for a ~A$3m upfront payment
Strong Cash and Funding Position Post Capital Raising
•
Raising of approximately A$70.0m via a two-tranche placement at an Offer Price of A$0.04 per share, representing a 17.6% premium to the closing price of
Radiopharm’s shares on 19 June 2024
•
•
Subject to shareholder approval, Executive Chairman, Paul Hopper, will be participating for A$3m under the Offer
Post completion of the capital raise, Radiopharm will have a pro forma cash balance of A$72.9m, which it expects will fully fund its current clinical programs
until the end of 2026
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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LANTHEUS STRATEGIC INVESTMENT
Lantheus Holdings Inc (LNTH.NASDAQ, market cap approximately US$5.5Bn) is a global
leader in the development, manufacture and commercialisation of diagnostic and
therapeutic radiopharmaceutical products with offices in Massachusetts, New Jersey,
Canada and Sweden.
Lantheus is investing ~A$7.5m into
Radiopharm
Shares to be acquired at
$0.05 per share. A ~57%
premium to the 5-day
VWAP
Lantheus will secure rights over two
early preclinical assets for a A$3m
upfront payment
Global rights for RAD 206
Development (TROP-2)
and RAD 502 (DUNP19) in
exchange for a A$3 million
upfront payment
Option to invest a further ~A$7.5m
within 6 months
Additional investment to
be made at $0.05 per
share. A ~57% premium to
the 5-day VWAP
* Subject to shareholder approval. Shares subscribed for by Lantheus will be escrowed for 12 months from
allotment date
* Assumes an AUD/USD exchange rate of $0.6670
“We are pleased to make a strategic
investment in RAD and partner with
them to further expand our
innovative pipeline.
Radiopharmaceutical theranostics
are changing the way cancer is
diagnosed and treated, yet we still
have more work to do and are
inspired to further advance this field
with these two preclinical oncology
assets.”
Brian Markison, Chief Executive Officer of
Lantheus
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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CASE STUDY: LANTHEUS STRATEGIC INVESTMENT IN PERSPECTIVE
THERAPEUTICS
•
•
On 9th January 2024, Lantheus announced it had entered into multiple strategic
agreements with Perspective Therapeutics, Inc. (NYSE:CATX)*
Perspective is a clinical stage radiopharmaceutical company with advanced treatment
applications for cancers throughout the body. *
•
Three assets currently completing a Phase 1/2a trial
Option to exclusively license
Perspective’s Pb212-VMT-⍺-NET and
an option to co-develop certain early
stage therapeutic candidates for an
aggregate upfront payment of US$28
million in cash
20.0
18.0
16.0
14.0
12.0
10.0
8.0
6.0
4.0
2.0
0.0
Strategic investment of
approximately US$33 million to
acquire approximately 19.9% of
Perspective
Perspective Therapeutics Share Price – YTD 2024
Announcement of strategic
partnership with Lantheus
* See Lantheus announcement here: https://lantheusholdings.gcs-web.com/news-releases/news-release-details/lantheus-expands-radiopharmaceutical-oncology-pipeline-strategic
* The performance of Perspective Therapeutics is not necessarily indicative of RAD’s future performance
* Share price chart as at 24 June 2024. Source: Capital IQ
Perspective share price ~+150%
since the beginning of 2024 and
the subsequent announcement
of a strategic partnership with
Lantheus in January 2024
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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GROWING INTEREST IN RADIOPHARMA DEAL SPACE (2018 TO PRESENT)
Selected Recent M&A Transactions
Selected Recent Strategic Agreements
• Lantheus/Perspective (‘24) - $61MM upfront/investment
• POINT/LLY (‘23) - $1.4B acquisition
• Roche/Genentech/PeptiDream (‘23) - $40MM upfront (PD)
• Bayer/Bicycle (‘23) - $45MM upfront (product)
• Bicycle/Novartis (‘23) - $50MM upfront (PD)
• Actinium/Immedica (‘22) - $35MM upfront/commercial
• Lantheus/POINT (‘22) - $260MM upfront (product)
Public companies: 14, $12B combined Cap
Private Companies: 25+, $5.4B combined Cap
• Mariana acquired by Novartis for US$1.0B (May ‘24)
• Fusion Pharmaceuticals acquired by AstraZeneca US$2.4B (March ‘24)
• RayzeBio, Inc acquired by Bristol Myer Squibb for US$4.1B
(December ‘23)
• POINT BioPharma acquired by Eli Lilly for US$1.4B
(October ‘23)
40+ public financings
raised >$3.5B
100+ Acquisitions or Alliances
Provided $37B in Payments
PD = product development. Strategic Agreements and Financing Deals = Biomedtracker, Oct 4 2023; Public companies market cap = Fact Set Research and Brookline Capital Market estimates: Oct 4
2023; Private company info: Pitchbook and Brookline Capital Market estimates: Oct. 1 2023
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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6
RADIOPHARMACEUTICALS DELIVER RADIATION DIRECTLY TO
CANCER CELLS
CANCER
CELL
LINKER
TARGET
TARGETING
MOLECULE
RADIOACTIVE
ISOTOPE
Building Blocks of
Radiopharmaceuticals
Considerations
Targeting Molecule
(high affinity small
molecule, peptide or
antibody)
Serum half-life, immunogenicity, tumor uptake
and retention, plasma clearance (especially via
renal system)
Radioactive Isotope
(imaging / therapeutic)
Target heterogeneity, tissue anatomy, desired
cross-fire effect, mechanism of cytotoxicity,
imaging properties
Linker
(joins targeting molecule
and radioactive isotope)
Stability, uptake in desired versus undesired
organs
Imaging
Therapeutics
SEE and measure disease
with radioactive isotopes
TREAT cancer with high
energy particle emitters
Imaging compounds precisely delivers radioactive
isotopes to detect and image cancer cells
Very high selectivity to cancer cells while
limiting damage to healthy tissues
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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EXPANDING RADIOPHARMACEUTICAL TARGETS AND INDICATIONS
Novel Radiopharmaceutical Targets With Validated Biology
beyond PSMA, SSTR2, FAPI
PD-L1, HER2, (nanobodies); αVβ6 Integrin (peptide), fatty acid synthase (small molecule)
Tuned Isotope Selection
Lu177 (beta), Ac225 (alpha), Tb161 (beta + Auger)
Optimized Binding Moieties
Supply Chain Enhancement
Nanobodies, high affinity peptides, small molecules
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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CLINICAL PIPELINE (Nanobodies, Peptide, Small Molecule)
PROGRAM
RAD204
RAD202
RAD301
RAD302
TARGET &
MOLECULE
PD-L1
(Nanobody)
HER 2
(Nanobody)
Integrin
αVβ6
(Peptide)
INDICATION
Dx/Tx
ISOTOPE
NON-SMALL CELL
LUNG CANCER
Therapy
Lu177
Phase 1 enrolling in Australia, NCT06305962
BREAST /
GASTRIC CANCER
Therapy
Lu177
Ethics approval in Q3 2024
Phase 1 trial starting in Q3-Q4 2024
Imaging
Ga68
Therapy
Lu177
PRECLINICAL
PHASE I
PHASE II
NOTES
FDA Orphan Drug Designation
Phase 1 enrolling in the US, NCT05799274
PANCREATIC
CANCER
Preclinical package to be completed by 2024
Phase 1 trial planned in early 2025
Phase 2a Phase 2b
RAD101
RAD102
Fatty Acid
Synthase
(Small Molecule)
Imaging
F18
IND preparation for Phase 2b in US (n=30)
Therapy
I123
Preclinical studies progressing
BRAIN METS
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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PRECLINICAL ASSETS
PROGRAM
TARGET &
MOLECULE
INDICATION
Dx/Tx
ISOTOPE
PROSTATE
Therapy
Tb161
PRECLINICAL
PHASE I
PHASE II
NOTES
KLK3
RAD402
(mAb)
CMC production ongoing, BioD study ongoing
(Phase 1 in 2025 depending on financials)
JV with MD Anderson
PROGRAM
TARGET &
MOLECULE
B7H3
RV01
(mAb)
INDICATION
Dx/Tx
ISOTOPE
Multiple
Indications
Therapy
Lu177
PRECLINICAL
PHASE I
PHASE II
NOTES
CMC production ongoing
Phase 1 planned in 1H 2025
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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Fully Funded To Achieve Upcoming Milestones, which is anticipated to include Four Read-Outs
1H 2024
PROGRAM
TARGET &
MOLECULE
INDICATION
Dx/Tx
ISOTOPE
RAD204
PD-L1
(Nanobody)
NON-SMALL CELL
LUNG CANCER
Therapy
Lu177
RAD202
HER 2
(Nanobody)
BREAST /
GASTRIC CANCER
Therapy
Lu177
Imaging
Ga68
Therapy
Lu177
Imaging
F18
Therapy
I123
RAD301
RAD302
RAD101
RAD102
Integrin
αVβ6
(Peptide)
Fatty Acid
Synthase
(Small Molecule)
PANCREATIC
CANCER
2H 2024
1H 2025
P1 in Aus
2H 2025
read-out
P1 in Aus
P1 in USA
1H 2026
read-out
read-out
P1 in USA
P2b in USA
read-out
BRAIN METS
P1 in USA
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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KEY MANAGEMENT TEAM
Paul Hopper
Riccardo Canevari
Chief Executive Officer
Vittorio Puppo
Chief Operating Officer
Dr. Sherin Al-Safadi
• Founder of Radiopharm
Theranostics
• Radiopharm Theranostics
CEO since September 2021
• 25 years experience as a
life-sciences entrepreneur
• Previously, Chief
Commercial Officer of
Novartis Company
Advanced Accelerator
Applications S.A.
• Has served as Chief
Operating Officer since
June 2022
• Served in the role since Aug
2023
• Served in the role since
September 2023
• Previously, VP Medical
Affairs at Point Biopharma
• Previously Vice President,
Head of CMC and Supply
Chain at Orum
Therapeutics
Executive Chairman
• Founder, Chairman, nonexecutive director or CEO
of more than fifteen
companies in the US,
Australia and Asia
• Previous and current
Boards include Imugene,
Chimeric Therapeutics,
Viralytics, Prescient
Therapeutics, Polynoma
and Arovella Therapeutics
• Lead for Lutathera inmarket growth strategy &
Pluvicto launch strategy
• Senior Vice President &
Global Head, Breast
Cancer Franchise,
for Novartis Oncology
since 2017
• Previously, Chief Marketing
Officer at Bracco Imaging,
a world leader in
diagnostics
• Managed businesses in
Europe and Asia for
Accuray, Covidien,
Mallinckrodt and
Amersham
• Board member of Life
Sciences Capital
Vimal Patel
VP, Medical Affairs
• Lead Strategic & Tactical
planning
radiopharmaceutical Phase
III programs
• Global Director, Medical
Affairs at Bayer
VP, CMC
• Led the successful
manufacture of two ADCs
and contributed to filing an
IND leading to a Phase-I
trial
• Director of Process
Sciences and
Manufacturing at Actinium
Pharmaceuticals
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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CLINICAL PIPELINE
(Nanobodies, Peptide, Small Molecule)
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD 204 Therapeutic: PD-L1 NANOBODY
PD-L1 NANOMAB
Single domain monoclonal antibody (Sd mAb)
CANCER CELL
TARGET
PD-L1
PD-L1 Immune Checkpoint Protein
Overexpression mediates evasion of immune
responses by cancer cells
Blockade by antibodies leads to tumour
regression
LINKER
TARGETING
MOLECULE
Sd mAb
RADIOACTIVE
ISOTOPE
99Tc to SEE
177Lu to TREAT
BENEFITS OF NANOBODY MOIETY
•
Provides the specificity of a full-size antibody; can
bind different epitopes than full-sized antibodies
•
Allows for more rapid tumor accumulation
•
Rapidly cleared from blood circulation
THERAPY
•
Strong potential as a preferred combination
partner with checkpoint inhibitors (overcome ICI
resistance + abscopal effect)
•
Proven targeting of different epitope vs
atezolizumab
•
PFE/Seagen PD-L1 ADC in development in
combination with ICI
•
Phase I data Pluvicto + pembrolizumab shows
promising results (synergistic effect in Prostate
Cancer) R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD 204 Therapeutic: PD-L1 NANOBODY
CLINICAL DEVELOPMENT & REGULATORY STRATEGY
•
Human pharmacokinetic and biodistribution validated with imaging agent (positive Phase I in 16 pts)
•
Phase I therapeutic dose escalation trial in Australia started
•
Phase II combo therapy trial with checkpoint inhibitor to follow
•
No other PD-L1-targeted radiopharmaceuticals in preclinical or clinical development
PRECLINICAL
√
Imaging PHASE I
Therapeutic PHASE I
PHASE II
16pts
27 pts
50 pts
√
Q1 2024– Q2 2025
Q4 2025 – Q3
2027
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD 204 (NM-01) Does Not Interfere With ICI Binding - Combination Potential
Binding kinetics at different doses with
or without the presence of atezolizumab
Biodistribution of [99mTC]-NM-01 in mice
180
Human PD-L1
Kd = 0.8 nM
Resp. Diff
130
80
30
200
400
600
800
Biodistribution at 30 min
1000
Time
%ID/g
250
200
Resp. Diff
150
2
100
50
0
(50)
Biodistribution at 90 min
250
200
150
100
50
3
2
1
1
0
0
NM-01
Atezo + NM-01
Atezo
(100)
(150)
(200)
0
250
200
150
100
50
3
%ID/g
(20)
0
100
200
300
400
500
600
700
800
Time
In vitro, our nanobody exhibited sub-nanomolar
affinity to human PD-L1 and atezo saturation has
no impact on its binding
Source: Wong et al. AJNMMI 2021; 11(3):154-156.
Note: NM-01 is our anti-PD-L1 sdAb
Group 1 – 37 MBq, 10ug NM-01
Group 2 – 37 MBq, 200ug NM-01
Group 3 – 37 MBq, 10ug NM-01 + 2 mg atezo
In vivo, atezo pre-treatment in mice does not reduce
NM-01’s tumor uptake when compared to
administration with NM-01 alone
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD 204 - Imaging with 99mTc
Favorable Biodistribution and Diagnostic Characteristics in NSCLC
Time–activity curves for organs with highest
99mTc-RAD204 uptake
Presence of intra-patient heterogeneity in PD-L1 expression between primary
tumor and nodal malignancies
•
PI FIH study: SPECT imaging of 16 NSCLC patients with 99mTc-labeled RAD 204 (NM-01)
•
Heterogeneity of PD-L1 expression between primary tumor and nodal sites of disease within same patient
•
•
PD-L1 expression detection by imaging is fast and noninvasive, and may be preferred compared to invasive IHC
No reported adverse reactions and acceptable radiation dosimetry
Xing Y. et al, J Nucl Med 2019;60:1213–1220
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD 204 TRIAL DESIGN
177Lu-anti-PD-L1 single domain Ab in metastatic non-small cell lung cancer
• Primary Objectives (Phase 1, Treatment):
• To assess the safety and tolerability of 177Lu-RAD204tr
• To determine the recommended dose(s) of 177Lu-RAD204tr for
future exploration
• Population: ≥ 18 years of age with a documented history of PD-L1
positive (>1%) metastatic NSCLC
Phase 0
(Imaging
Period with
177LuRAD204im)
• Design Methodology: BOIN for escalation / de-escalation. N=23
• Imaging: Imaging and dosimetry with low dose 177Lu-RAD204im,
consisting of 177Lu-RAD204im Safety Lead-in, with or without dose
escalation.
• Therapeutic Dose: 177Lu-RAD204tr dose escalation. Treatment
period of up to 3 cycles every 6 weeks.
Phase I
(Treatment
Period with
177LuRAD204tr)
Dose Level1
Dose (mCi)
Dose (GBq)
Imaging
dose
10
0.37
Dose Level2
Dose (mCi)
Dose (GBq)
DL1
30
1.1
DL2
40
1.5
DL3
TBD
TBD
DL4
TBD
TBD
• Estimated Time to Primary Completion: ~15 months
• Dosimetry (Phase 0, Imaging): To assess the biodistribution,
pharmacokinetics and radiation dosimetry of 177Lu-RAD204im in
selected organs and tumor lesions.
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD 202 Therapeutic: HER-2 NANOBODY
HER-2 NANOMAB
Single domain monoclonal antibody (Sd mAb)
CANCER CELL
TARGET
HER2
HER-2 pathway validated in Oncology.
Overexpression in Breast Cancer and
Gastroesophageal cancers
LINKER
TARGETING
MOLECULE
Sd mAb
RADIOACTIVE
ISOTOPE
99Tc to SEE
177Lu to TREAT
BREAST & GASTRIC HER2+ THERAPY FOR PATIENTS REFRACTORY TO ENHERTU
Why Post-Enhertu Market Is Increasingly Attractive
•
Enhertu is moving up treatment lines (DESTINY-BREAST trial)
•
DAISY trial demonstrated Enhertu activity in HER2-low and undetectable breast cancer patients
•
No established post-Enhertu therapy
•
Increasing HER2-low identification efforts to incorporate more patients
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD 202 Therapeutic: HER-2 NANOBODY
CLINICAL DEVELOPMENT & REGULATORY STRATEGY
•
Human pharmacokinetic and biodistribution proven with imaging agent (positive Phase I in 10pts in 2021, followed by
IIT in Germany in additional 6 pts.
•
99mTc-labeled single-domain antibody for SPECT/CT assessment of HER2 expression demonstrated favorable safety for
use in breast cancer imaging, with reasonable radiation doses, biodistribution and imaging characteristics (Zhao, et al.
Molecular Pharmaceutics)
•
Preclinical package and CMC completed; clinical protocol finalized
•
Phase I therapeutic dose escalation in Breast / Gastric Cancers planned in Australia in H2 2024
PRECLINICAL
√
Imaging PHASE I
PHASE I
PHASE II
10pts + IIT in 6pts
21 pts
50 pts
√
H2 2024 – H1 2026
H1 2026 – H2 2027
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD202 - 99mTc SPECT Imaging of Breast Cancer Patients to Determine HER2 Status
Favorable Biodistribution and Diagnostic Characteristics
Varied uptake of 99mTc-RAD202 in primary and metastatic lesions (CT – top)
and SPECT/CT (bottom), demonstrating heterogeneity of HER2 expression
Time–activity curves for organs
•
PI FIH study: SPECT imaging with 99mTclabeled RAD 202 (NM-02) to detect HER2 status
of 10 breast cancer patients
•
Rapid clearance of 99mTc-RAD204 from liver,
spleen, and intestines 1 h after injection
•
No reported adverse reactions and acceptable
radiation dosimetry
Zhao L, et al. Mol Pharm. 2021 Sep 6;18(9):3616-3622
• Accumulation of 99mTc-RAD204 observed in
metastases with varying degrees of uptake
• Intra- and inter-tumoral heterogeneity in
HER2 expression highlights need for
noninvasive imaging to drive treatment
decisions
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
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RAD 202 - TRIAL DESIGN
HEAT Trial (HER2 Antibody Therapy with Lutetium-177) in patients with HER2+ advanced solid tumors
• Primary Objectives (Phase 1, Treatment):
• To assess the safety and tolerability of 177Lu-RAD202tr
• To determine the recommended dose(s) of future
exploration for 177Lu-RAD202
• Population: Advanced solid tumours with HER2
amplification by local testing, including IHC,FISH and/
NGS
• Design Methodology: TITE-BOIN to support the doseescalation of 177Lu-RAD202 to allow continuous accrual
and real-time dose assignment for new participants. N=21
Phase 0
(Imaging Period
177
Lu-RAD202im)
with
Phase I
(Treatment Period with
177
Lu-RAD202tr)
Dose Level
Imaging
dose
Dose Level2
Dose (mCi)
10 mCi
Dose (mCi)
%Change
levels
in
DL1
~1.1 GBq (30
mCi)
+0%
• Imaging: 177Lu-RAD202im, consisting of 177Lu-RAD202im
Safety Lead-in, with or without dose escalation.
DL2
~2.2 GBq (60
mCi)
+100%
• Therapeutic Dose: 177Lu-RAD202tr dose escalation.
Treatment period of up to 3 cycles every 6 weeks.
DL3
~4.4 GBq
(120mCi)
+100%
DL4
~6.6 GBq (180
mCi)
+50%
DL5
~8.8 GBq (240
mCi)
+33.33%
• Estimated Time to Primary Completion: ~12-18 months
• Dosimetry (Phase 0, Imaging): To assess the
biodistribution, pharmacokinetics and radiation
dosimetry of 177Lu-RAD202im in selected organs and
tumour lesions.
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
dose
22
RAD 301/302 : Imaging and Therapy for Pancreatic Cancer
TRIVEHEXIN
RGD peptide (arginylglycylaspartic acid)
Integrin αvβ6 receptor antagonist
CANCER CELL
TARGET
integrin αvβ6
LINKER
TARGETING
MOLECULE
trivehexin
RADIOACTIVE
ISOTOPE
68Ga to SEE
177Lu to TREAT
INTEGRIN αvβ6
•
Design features include hydrophilicity to reduce nonspecific uptake into undesired organs and increase
clearance in plasma, trimerization to increase affinity,
cyclicity for better selectivity, uptake and tumor retention
Target often referred to as “the cancer integrin” given
its role in activation of TGFβ and resultant
immunosuppression; Expression correlates with
decreased survival in numerous carcinomas
•
Pliant Phase IIa data validates the target in Lung and
Liver Fibrosis
•
PFE/Seagen αvβ6 integrin planning Phase III in NSCLC
THERAPY FOR αvβ6 INTEGRIN EXPRESSING TUMORS
•
Pancreatic cancer is the first targeted indication (~60%
expression)
•
Multi-indication potential beyond PDAC (Head & Neck, NSCLC,
TNBC, Colorectal)
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
23
RAD 301 Imaging: Ga68-Integrin αVβ6
CLINICAL DEVELOPMENT & REGULATORY STRATEGY
•
66 patients already dosed under compassionate use (No drug-related adverse events reported)
•
33 patients dosed under Investigator Initiated Research (presented at EANM 9/2023)
•
IND approved Phase I started, plans to leverage Real-World Evidence and seek a registrational
trial
•
USD 240m peak yearly sales potential in Imaging PDAC (Bell Potter independent report)
•
Only 1 expected competitor: Integrin αvβ6 - αvβ1 (UC Davis) currently in Phase I
COMPASSIONATE
USE (Germany)
Pilot study in PDAC +
H&N
PHASE I
66 pts
33pts
9 pts
~100 pts
√
√
READ OUT in
2024
1H 2025 – 1H 2026
PHASE II
PHASE III
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
24
RAD301 Clinical Development (Imaging)
68Ga-trivehexin PET/MRI Imaging Patients with
Pancreatic Tumors
•
•
•
Selective detection of αvβ6 integrin-expressing tumour lesions in
patients with PDAC
66 patients administered RAD301 (as of 2022)
– 60 pancreatic cancer and GI tumours
– 5 with head and neck cancer
– 1 patient with tumour of unknown origin
Results indicate that RAD301 can be used to detect and monitor
pancreatic cancer
– Rapid and specific accumulation in many target PDAC
primary lesions and metastases
– Low background accumulation and purely renal elimination
68Ga-trivehexin PET/CT Imaging vs F18-FDG
•
•
•
Selective detection of αvβ6 integrin-expressing tumor lesions in
patients with PDAC & HNSCC
33 patients administered RAD301
Results indicate that RAD301 shows incremental value over
F18-FDG in PDAC & HNSCC
– Favorable tumor-to-background contrast vs F18-FDG
– Sharper images and negligible uptake in the surrounding
normal tissue
68Ga-trivehexin PDAC imaging shows
superior resolution vs F18-FDG
68Ga-TRIVEHEXIN PDAC IMAGING
Partnered with TRIMT
Quigley NG Notni J. Eur J
Nucl Med 2021
Partnered with TRIMT
Data presented at World Theragnostic Congress 2022 (Wiesbaden, Germany) & follow up
presented at EANM 9/2023 (Vienna)
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
25
MULTI-INDICATION POTENTIAL BEYOND PANCREATIC CANCER
Expression of αvβ6-integrin in
human cancers
High expression case studies
NSCLC (103 cases, 291 specimens)
ESCC (100 cases, 306 specimens)
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
26
RAD 302 Therapeutic: Lu177-Integrin αVβ6
CLINICAL DEVELOPMENT & REGULATORY STRATEGY
•
GMP peptide production ongoing
•
GLP Tox and Biodistribution study planned in 2024
•
IND submission in H2 2024
•
Next step: Phase I dose escalation basket trial (multiple indications) planned for early 2025
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
27
RAD 101: Imaging and Therapy for Brain Metastases
F18-PIVALATE
CANCER CELL
TARGET
Fatty acid
oxidation
Selectively targets fatty acid synthase
which is overexpressed in tumours but
not normal brain cells
LINKER
TARGETING
MOLECULE
pivalate
RADIOACTIVE
ISOTOPE
18F to SEE
131I / 123I / 211At to TREAT
THERAPY
FATTY ACID SYNTHASE IS A VIABLE TARGET
•
•
Upregulation of de novo fatty acid synthesis via
FASN enables cancer cells to grow in the lipidderived microenvironment of the brain
•
R&D stage for candidate selection at Imperial
College of London
•
Isotope selection based on chemical stability
Disruption of FASN activity can impair growth of
brain metastases, representing a viable
therapeutic target
•
Potential use beyond brain mets (e.g., gliomas)
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
28
RAD 101 Imaging: F18-PIVALATE
CLINICAL DEVELOPMENT & REGULATORY STRATEGY
•
Ongoing Tech transfer from UK to USA. IND approval after Tech transfer finalized
•
24 months to complete late-stage development (Phase IIb + Phase III)
•
Only 1 expected competitor: Axumin (Bracco) currently in Phase III
PRECLINICAL
√
PHASE I
PHASE IIa
PHASE 2b
PHASE 3
24 pts
17 pts
30 pts
150 pts
√
√
2H 2024-1H 2025
2H 2025 – 2H2026
R A DIO P H A R M TH E R A N O STIC S L TD 20 24
29
RAD 101 Delivers Positive Phase II
Data in Brain Metastasis Trial
RAD101 Phase IIa Clinical Trial:
F18-p
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