FORE Biotherapeutics · Competitive Intelligence

BRAF and pan-RAF discontinuations — who stopped, and why

Every company that has halted, deprioritised, divested or written off a BRAF or pan-RAF inhibitor programme, with the reason each one actually gave. A companion cut to the plixorafenib competitive-intelligence hub, organised by cause of death rather than by competitor.

Data cut · 24 Aug 2026 Public sources · cited 10 sponsor decisions · 11 assets Draft — open flags at the end
Provenance. Everything on this page is public and cited — company press releases, SEC filings, regulator-facing pipeline updates, ClinicalTrials.gov records and peer-reviewed papers. No plixorafenib figures appear here; where the read-across touches Fore's own programme it is stated qualitatively and points back to internal sources. Reasons are reported as the sponsor stated them; where a sponsor gave no reason, the row says so rather than inferring one.
The finding

Not one BRAF or pan-RAF programme in this set was stopped because the mechanism failed on safety. Of ten sponsor decisions, seven were portfolio or capital-allocation calls — the asset was fine, the company changed shape around it. Two were efficacy shortfalls, both in first-generation compounds a decade old. One was a tolerability failure of a specific combination, not of the RAF agent alone.

The second finding matters more commercially: the asset usually outlives the decision. Five of the ten dropped programmes were picked up by someone else and are still in development — and one of them, tovorafenib, went on to become the only FDA-approved drug in the class. Plixorafenib is itself a survivor of exactly this pattern, having outlived the closure of Plexxikon.

10
sponsor decisions to stop, deprioritise or divest a BRAF / pan-RAF programme
7
driven by portfolio reprioritisation or capital constraint
2
driven by an efficacy shortfall — both pre-2015 compounds
1
driven by tolerability — a combination arm, not the RAF agent alone
5
assets that survived the sponsor's exit and are still in development elsewhere
0
stopped for a class-wide safety signal
1The register

Ordered by recency of the decision. "Reason" is the sponsor's stated rationale, not our inference. "Asset today" records whether the molecule is still being developed by anyone.

AssetSponsor that stoppedClassStage when stopped Decision & dateStated reasonCategoryAsset today
NaporafenibLXH254 · ERAS-254 Erascalicensed from Novartis Pan-RAF Phase 3 (SEACRAFT-2) Strategic review May 2025 → sought a partner; termination notice to Novartis Mar 2026, effective 3 Jun 2026 Prioritise the RAS-targeting franchise (ERAS-0015, ERAS-4001); extend runway from H2 2027 to H2 2028. No efficacy or safety rationale stated publicly. Portfolio Rights reverted to Novartis
DCC-3084brain-penetrant RAF dimer inhibitor Deciphera / Ono Pan-RAF Phase 1/2 US development discontinued Sep 2025 Strategic reasons — explicitly not safety or efficacy, per the sponsor. Portfolio Stopped in the US
BDTX-4933 Black Diamond Therapeutics RAF (pan-RAF / BRAF) Phase 1 Deprioritised in a restructuring Oct 2024; licensed to Servier Mar 2025 ($70M upfront, up to $710M milestones) Concentrate resources on BDTX-1535 (EGFR) and extend cash runway; actively sought a partner for the RAF asset. Portfolio Live — Servier
BelvarafenibHM95573 · RG6185 Genentech / Rochelicensed from Hanmi 2016 Pan-RAF (type II) Phase 1b / basket Removed from the Roche portfolio 2024; enrolment stopped in two studies, enrolled patients continued on treatment Broad portfolio reset — Roche cut roughly 20% of its new molecular entities, focusing on assets with a "lower likelihood" of success. Portfolio Live — Hanmi (Korea)
BrimarafenibBGB-3245 — combination arm only MapKureBeiGene / SpringWorks JV BRAF (next-gen) Phase 1 combination Trial BGB-3245-AU-001 terminated Jan 2025 Lack of tolerability of brimarafenib given in combination with mirdametinib. Monotherapy and other combinations continued. Tolerability Live — other trials
ExarafenibKIN-2787 Kinnate Biopharma Pan-RAF Phase 1 Sold to Pierre Fabre 5 Mar 2024; Kinnate acquired by XOMA and wound down (Apr 2024) Company-level pursuit of strategic alternatives. Pierre Fabre assumed 100% of programme costs and cited a potential best-in-class profile. Portfolio Live — Pierre Fabre
PLX8394now plixorafenib Daiichi Sankyo / Plexxikon BRAF "paradox breaker" Phase 1/2 (already out-licensed) Plexxikon R&D unit closed 31 Mar 2022 (announced Jan 2022, ~60 staff) Daiichi Sankyo R&D reorganisation to concentrate on three ADCs — Enhertu, Dato-DXd, HER3-DXd. Portfolio Live — Fore Biotherapeutics
TovorafenibTAK-580 · MLN2480 · DAY101 Takeda / Millennium Pan-RAF (type II) Phase 1 (adults) Adult development ceased; out-licensed to Day One, agreement effective 16 Dec 2019 Adult-oncology strategy; internal paediatric advocates pushed for an out-licence rather than a shelf. Portfolio Approved — Ojemda, Apr 2024
LY3009120DP-4978 Eli Lilly Pan-RAF / RAF dimer Phase 1 Discontinued after the first-in-human study Lack of clinical efficacy — unexpected, since exposures reached levels predicted to be therapeutic from preclinical work. Efficacy Discontinued
RAF265CHIR-265 Novartis RAF / VEGFR-2 Phase 1/2, melanoma Phase 2 dose-expansion cancelled by protocol Amendment 7, Dec 2011; study completed Nov 2013 Modest single-agent activity — 8 of 66 evaluable patients responded (12.1%) at an MTD of 48 mg daily. Efficacy Discontinued
LifirafenibBGB-283 BeiGene / BeOne Medicines BRAF monomer + dimer Phase 1b combination No public discontinuation statement. Combination study NCT03905148 shows COMPLETED as of Jan 2026 None given. Lifirafenib was not among the five oncology assets BeOne cut in May 2026. Programme appears dormant rather than formally stopped. Unresolved Status unclear
Read the last row carefully. Lifirafenib is the one entry where we could not find a sponsor statement either way. It is listed because its absence from the register would be misleading, not because a discontinuation is established. Treat it as an open question, not a finding — see the open flags.
2Grouped by cause

A · Portfolio reprioritisation and capital allocation — seven of ten

The dominant mode by a wide margin. In every one of these cases the sponsor's public rationale was about the shape of its own pipeline or balance sheet, and in five of the seven the asset was deliberately placed with someone else rather than shelved.

Erasca → naporafenib

Pan-RAF · in-licensed from Novartis · stopped at Phase 3

The most consequential recent exit, because it removed a Phase 3 pan-RAF asset from the competitive set. Erasca ran a strategic pipeline review in May 2025 as ERAS-0015 (pan-RAS molecular glue) and ERAS-4001 (pan-KRAS) approached the clinic, decided to seek a partner for naporafenib, and when none materialised served notice on Novartis in March 2026, terminating effective 3 June 2026. The stated driver was focus and runway — extending cash from H2 2027 to H2 2028.

What was not said: Erasca has not publicly attributed the decision to SEACRAFT-2 Stage 1 data. Stage 1 randomised data had been guided for H2 2025 and we could not locate a public readout. Whether the data informed the call is unresolved and is flagged below — it should not be assumed either way.

Genentech / Roche → belvarafenib

Type II pan-RAF · licensed from Hanmi for $80M upfront in 2016 · stopped at Phase 1b

Caught in Roche's broad portfolio reset, which cut roughly a fifth of its new molecular entities on a "lower likelihood of success" screen. Genentech stopped enrolment in two studies and removed the asset from the portfolio, while continuing to treat and monitor patients already enrolled — the standard responsible-exit pattern, and a useful signal that this was not a safety action.

The asset lived. Hanmi retained Korean rights throughout and Korean regulators cleared a Phase 2 of belvarafenib plus cobimetinib in NRAS-mutant melanoma on 5 January 2026 — the same combination a Fore KOL characterised as previously failed. Worth noting that the combination is being retried by the originator, not abandoned.

Kinnate → exarafenib

Pan-RAF · Phase 1 · sold, then the company was wound down

A company failure rather than an asset failure, and the distinction matters for how the exit reads. Kinnate announced a search for strategic alternatives, sold exarafenib and the rest of the pan-RAF programme to Pierre Fabre on 5 March 2024 — closing on signing, with Pierre Fabre taking on 100% of programme costs and $30.5M in contingent milestones tied to dosing in a first pivotal trial — and was then acquired by XOMA, which wound down operations.

Read-across: Pierre Fabre bought it precisely because it thought the profile might be best-in-class, and the milestone structure implies a pivotal trial was contemplated. This is an acquirer's vote of confidence in the mechanism, recorded at the moment a sponsor was exiting it.

Black Diamond → BDTX-4933

RAF · Phase 1 · deprioritised, then licensed on

Deprioritised in an October 2024 restructuring to concentrate on the EGFR asset BDTX-1535 and fund operations into Q2 2026, with the company saying openly that it was seeking a partner. Servier took it five months later for $70M upfront and up to $710M in milestones. Phase 1 data has since slipped to late 2026 or early 2027.

Pattern: the second case in this register where a cash-constrained small-cap deprioritised a RAF asset and a European pharma paid meaningfully for it within months.

Deciphera / Ono → DCC-3084

Brain-penetrant RAF dimer inhibitor · Phase 1/2 · US development stopped Sep 2025

The cleanest statement of cause in the whole register: dropped for strategic reasons, with the sponsor explicitly ruling out safety and efficacy. It followed Ono's $2.4B acquisition of Deciphera in April 2024, which is the more likely proximate driver — an acquirer rationalising an inherited early pipeline.

Relevance to Fore: DCC-3084 was brain-penetrant and MAPK-pathway directed — the nearest mechanistic neighbour in this register to plixorafenib's CNS positioning. Its removal takes a CNS-capable RAF dimer inhibitor out of the US competitive set for reasons unrelated to whether it worked.

Takeda → tovorafenib

Type II pan-RAF · adult development ceased 2019 · out-licensed to Day One

The single most instructive case in the class. Takeda stopped developing TAK-580 in adults around 2019; rather than shelving it, internal paediatric advocates pushed for an out-licence, and the agreement with Day One took effect on 16 December 2019. In April 2024 the same molecule won FDA accelerated approval as Ojemda in relapsed/refractory paediatric low-grade glioma.

The lesson the register keeps repeating: a discontinuation decision is a statement about a sponsor's strategy, not a verdict on a molecule. The only approved drug in this class is one a large pharma discontinued.

Daiichi Sankyo → Plexxikon (and with it, PLX8394)

BRAF paradox breaker · the origin of plixorafenib

Daiichi Sankyo announced an R&D reorganisation in January 2022 and closed the Plexxikon unit — roughly 60 people — on 31 March 2022, to concentrate on Enhertu, Dato-DXd and HER3-DXd. PLX8394 had already been licensed worldwide to Novellus, now Fore Biotherapeutics, in June 2020.

Direct relevance: Fore's lead asset exists because of a portfolio exit of exactly the kind catalogued on this page. When a competitor's programme is dropped for strategic reasons, the base rate says the molecule finds another home — this company is the proof.

B · Efficacy shortfall — two of ten, both first-generation

Eli Lilly → LY3009120

Pan-RAF / RAF dimer inhibitor · discontinued after first-in-human

The clearest genuine efficacy failure in the class. The Phase 1 publication records that the absence of clinical activity was unexpected given strong preclinical efficacy and pharmacokinetic exposures at levels predicted to be therapeutic in RAS- and RAF-mutant tumours.

Why it does not generalise: the gap was between preclinical prediction and clinical exposure–response for that compound. It is a caution about translating preclinical potency, not evidence against RAF dimer inhibition as a strategy — a distinction later type II agents, tovorafenib above all, have borne out.

Novartis → RAF265

RAF / VEGFR-2 dual inhibitor · Phase 2 expansion cancelled Dec 2011

The first-in-human study enrolled melanoma patients irrespective of BRAF mutation status and produced responses in 8 of 66 evaluable patients (12.1%) at an MTD of 48 mg once daily. The Phase 2 dose-expansion was cancelled by protocol amendment in December 2011 and the study closed in November 2013.

Design, as much as molecule: a dual RAF/VEGFR agent tested in an unselected population is close to the opposite of the selection strategy the class now uses. It reads today as a patient-selection failure at least as much as a mechanism failure.

C · Tolerability — one of ten, and only in combination

MapKure → brimarafenib plus mirdametinib

BGB-3245 · BeiGene / SpringWorks joint venture · trial terminated Jan 2025

Trial BGB-3245-AU-001 was terminated for lack of tolerability of brimarafenib when given in combination with mirdametinib. Brimarafenib itself continued in other studies, including a combination with panitumumab in RAS-mutant colorectal and pancreatic cancer.

The relevant read: this is a RAF + MEK vertical-combination tolerability problem, which is a recurring theme across the MAPK field, rather than a signal against the RAF agent. It is the only tolerability-driven stop in the register and it did not end the programme.

D · Unresolved

BeiGene / BeOne → lifirafenib

BGB-283 · BRAF monomer and dimer inhibitor · status unclear

Lifirafenib does not appear in BeOne's May 2026 cull, which covered BG-60366 (EGFR), BGB-53038 (pan-KRAS), BG-89894 (MAT2A), BG-68501 (CDK2) and the CCR8 antibody BGB-A3055. The lifirafenib plus mirdametinib study NCT03905148 is recorded as completed as of January 2026, and we found no sponsor statement about the programme's future.

Disposition: carried as unresolved. Asserting a discontinuation from the absence of activity would be exactly the inference this page is written to avoid. Needs a direct check of BeOne's current pipeline page and most recent earnings materials.
3Two corrections to the competitive-intelligence hub

Sourcing this page surfaced material discrepancies against Competitive_Intelligence_REVIEW.html. They are flagged here, not silently rewritten there.

What the hub saysWhat the public record showsSeverity
Mosperafenib · RG-6344 listed as "Roche (discontinued, out-licensing)" in the Tier 2 basket watchlist Roche has not discontinued it. Mosperafenib (RG6344 / RO7276389) is in active Phase 1 dose escalation as monotherapy and with cobimetinib, with data presented at AACR and ASCO 2025 — a 24.2% ORR in BRAF V600E-mutant solid tumours and no class cutaneous toxicities reported. The hub's own source list cites that readout, so the status label contradicts its own evidence. Medium
Naporafenib tracked as an active Erasca Phase 3 (SEACRAFT-2) asset Superseded. Erasca stopped development and terminated the Novartis licence effective 3 June 2026; rights have reverted. The asset should move from the tracked set to this register. High
Also worth a check. The hub carries a belvarafenib TAPISTRY Phase 2 readout at 09/2031. Given Genentech stopped enrolment and removed the asset in 2024, that timeline should be reconciled against the current TAPISTRY record before it is quoted anywhere.
4What this means for plixorafenib

Four conclusions that follow from the register, stated at the level the evidence supports.

  1. There is no class safety story to defend against. Across a decade and eleven assets, no BRAF or pan-RAF programme in this register was stopped for a mechanism-level safety signal. Diligence questions that imply a class liability are not supported by the discontinuation record, and this page is the citation set for saying so.
  2. The real class risk is commercial, not scientific. Seven of ten exits were portfolio or financing decisions. That is a statement about how sponsors behave under capital pressure, and it applies to every small-cap in the field — a risk of the ownership structure, not of the target.
  3. Competitive attrition is not competitive clearance. Five of these assets are still in development under new owners — Pierre Fabre, Servier, Hanmi, Day One and Fore. Treating a sponsor exit as the removal of a competitor is the error the tovorafenib history most sharply warns against.
  4. The CNS-directed field just got thinner for non-scientific reasons. DCC-3084's US stop removed a brain-penetrant RAF dimer inhibitor for strategic reasons, and naporafenib's Phase 3 exit removed the most advanced pan-RAF competitor. Neither was an efficacy verdict, so neither should be scored as validation of Fore's position — but both change the near-term landscape.
Guardrail. No plixorafenib efficacy, safety or exposure figure appears anywhere on this page. Any comparison to Fore's own data must be completed by the team from cleared internal sources, with CNS response reported in RANO / RAPNO / iRANO and denominators shown — per the CI process guardrails.
5Open flags — resolve before external use
  1. Lifirafenib status. No sponsor statement located. Check BeOne's current pipeline page and the most recent earnings deck before this row is cited anywhere.
  2. Naporafenib and SEACRAFT-2 Stage 1. Stage 1 randomised data was guided for H2 2025; we could not find a public readout. Whether data informed the termination is unknown and must not be asserted.
  3. Roche cull scope. The 20%-of-NMEs figure and the "lower likelihood of success" wording come from trade reporting of Roche statements, not a Roche primary document. Confirm against Roche's pipeline disclosure before quoting the percentage externally.
  4. RAF265 and LY3009120 provenance. Both efficacy conclusions rest on the Phase 1 publications rather than sponsor discontinuation notices. Accurate as characterisations of the data; they should not be quoted as formal corporate discontinuation statements.
  5. Completeness. This register covers assets that reached the clinic and had a locatable public decision. Preclinical terminations and undisclosed shelvings are out of scope by necessity — the count of ten is what the public record supports, not a claim about everything that happened.
6Sources
  1. Erasca, Inc. — Form 10-K for FY2025, naporafenib licence termination. sec.gov
  2. Erasca — "Early Clinical Advancement and Prioritization of RAS-Targeting Franchise." investors.erasca.com
  3. FierceBiotech — "Erasca enters another era, seeks partner for phase 3 ex-Novartis asset." fiercebiotech.com
  4. FierceBiotech — "Roche's pipeline rethink hits 20% of new molecules as cancer candidates join discard pile" (belvarafenib). fiercebiotech.com
  5. BioPharma Dive — "Genentech commits $80M upfront in Hanmi licensing deal." biopharmadive.com
  6. Korea Biomedical Review — Hanmi Phase 2 belvarafenib + cobimetinib clearance, NRAS-mutant melanoma. koreabiomed.com
  7. Pierre Fabre — acquisition of exarafenib from Kinnate Biopharma, 5 March 2024. pierre-fabre.com
  8. XOMA Royalty — agreement to acquire Kinnate Biopharma; closing of tender offer. investors.xoma.com
  9. Black Diamond Therapeutics — "Restructuring Plan to Focus Resources on BDTX-1535," 7 October 2024. investors.blackdiamondtherapeutics.com
  10. FierceBiotech — "Servier pays $70M to polish Black Diamond's deprioritized solid tumor prospect." fiercebiotech.com
  11. FierceBiotech — "Ono's Deciphera drops early-stage solid tumor drug for strategic reasons" (DCC-3084). fiercebiotech.com
  12. Ono Pharmaceutical — Financial Results 2Q (Apr–Sep) FY2025, pipeline changes. ono-pharma.com
  13. Daiichi Sankyo — "Announces Reorganization of R&D Structure," 12 January 2022 (Plexxikon closure). daiichisankyo.com
  14. Businesswire / Fore Biotherapeutics — Novellus exclusive worldwide licence for PLX8394, June 2020. businesswire.com
  15. Day One Biopharmaceuticals / Millennium (Takeda) — Asset Transfer and License Agreement, effective 16 December 2019. contracts.justia.com
  16. Springer, Drugs — "Tovorafenib: First Approval." link.springer.com
  17. Day One Biopharmaceuticals — "Giving New Life to Medicines and Options to Patients" (Takeda out-licence background). dayonebio.com
  18. Molecular Cancer Therapeutics — "A Phase I Study of LY3009120, a Pan-RAF Inhibitor, in Patients with Advanced or Metastatic Cancer." aacrjournals.org
  19. PMC — first-in-human Phase I of RAF265 in locally advanced or metastatic melanoma. ncbi.nlm.nih.gov
  20. ClinicalTrials.gov — NCT00304525 (RAF265, melanoma). clinicaltrials.gov
  21. ClinicalTrials.gov — NCT03905148 (lifirafenib + mirdametinib). clinicaltrials.gov
  22. AdisInsight — brimarafenib (BGB-3245) programme record, including terminated combination trial. adisinsight.springer.com
  23. Endpoints News — "BeOne culls five cancer programs and an autoimmune Phase 2." endpoints.news
  24. Pfizer — Q2 2026 pipeline update, 4 August 2026 (claturafenib, Phase 1). pfizer.com
  25. AACR Cancer Research — Abstract CT017, Phase I of RG6344 (mosperafenib) in BRAF V600-mutant solid tumours. aacrjournals.org
  26. Internal — Fore/competitive_intelligence/Competitive_Intelligence_REVIEW.html, the plixorafenib CI hub, and CI_PROCESS.md.
💬 Discussion